PMID
Article Title
Citation
Organization
Download
View Data
Identification of lactate as a driving force for prostanoid transport by prostaglandin transporter PGT.
Am J Physiol Renal Physiol 282: 1097-102 (2002)
Albert Einstein College Of Medicine
Solid-phase synthesis of FKBP12 inhibitors: N-sulfonyl and N-carbamoylprolyl/pipecolyl amides.
Bioorg Med Chem Lett 12: 1429-33 (2002)
Guilford Pharmaceuticals
Use of parallel-synthesis combinatorial libraries for rapid identification of potent FKBP12 inhibitors.
Bioorg Med Chem Lett 12: 1421-8 (2002)
Guilford Pharmaceuticals
Aromatic farnesyl diphosphate analogues: vinyl triflate-mediated synthesis and preliminary enzymatic evaluation.
Bioorg Med Chem Lett 12: 1417-20 (2002)
Wayne State University
Identification of potent and selective oxytocin antagonists. Part 2: further investigation of benzofuran derivatives.
Bioorg Med Chem Lett 12: 1405-11 (2002)
Glaxosmithkline
Identification of potent and selective oxytocin antagonists. Part 1: indole and benzofuran derivatives.
Bioorg Med Chem Lett 12: 1399-404 (2002)
Glaxosmithkline
Synthesis and biological activity of selective pipecolic acid-based TNF-alpha converting enzyme (TACE) inhibitors.
Bioorg Med Chem Lett 12: 1387-90 (2002)
Pfizer
Syntheses and bioactivities of novel carbamates combining platelet activating factor (PAF) receptor antagonist with thromboxane synthase inhibitor (TxSI).
Bioorg Med Chem Lett 12: 1383-6 (2002)
Nikken Chemicals
Synthesis of highly potent and selective hetaryl ureas as integrin alpha(V)beta3-receptor antagonists.
Bioorg Med Chem Lett 12: 1379-82 (2002)
Basf
Shikonin derivatives: synthesis and inhibition of human telomerase.
Bioorg Med Chem Lett 12: 1375-8 (2002)
Chinese Academy Of Science
Structure-based design of peptidomimetic antagonists of p56(lck) SH2 domain.
Bioorg Med Chem Lett 12: 1365-9 (2002)
Roche Products
Discovery and initial SAR of imidazoquinoxalines as inhibitors of the Src-family kinase p56(Lck).
Bioorg Med Chem Lett 12: 1361-4 (2002)
Bristol-Myers Squibb Pharmaceutical Research Institute
Bicyclic piperazinylbenzenesulphonamides are potent and selective 5-HT6 receptor antagonists.
Bioorg Med Chem Lett 12: 1357-60 (2002)
Glaxosmithkline
Design, synthesis and biochemical evaluation of AC ring mimics as novel inhibitors of the enzyme estrone sulfatase (ES).
Bioorg Med Chem Lett 12: 1343-6 (2002)
Kingston University
A novel type of nonsteroidal estrone sulfatase inhibitors.
Bioorg Med Chem Lett 12: 1339-42 (2002)
Hans-Kn�Ll Institute Of Natural Products Research
Discovery of phenyl alanine derived ketoamides carrying benzoyl residues as novel calpain inhibitors.
Bioorg Med Chem Lett 12: 1335-8 (2002)
Abbott
Structure-based optimisation of 2-aminobenzylstatine derivatives: potent and selective inhibitors of the chymotrypsin-like activity of the human 20S proteasome.
Bioorg Med Chem Lett 12: 1331-4 (2002)
Novartis Pharma
Design and synthesis of a piperazinylalkylisoxazole library for subtype selective dopamine receptor ligands.
Bioorg Med Chem Lett 12: 1327-30 (2002)
Institute Of Science And Technology
Design and synthesis of a novel series of 1,2-disubstituted cyclopentanes as small, potent potentiators of 2-amino-3-(3-hydroxy-5-methyl-isoxazol-4-yl)propanoic acid (AMPA) receptors.
J Med Chem 45: 2101-11 (2002)
Nps Allelix
Adenine nucleotide analogues locked in a Northern methanocarba conformation: enhanced stability and potency as P2Y(1) receptor agonists.
J Med Chem 45: 2090-100 (2002)
National Institute Of Diabetes
Structure-activity relationships of a novel class of endothelin-A receptor antagonists and discovery of potent and selective receptor antagonist, 2-(benzo[1,3]dioxol-5-yl)-6-isopropyloxy-4-(4-methoxyphenyl)-2H-chromene-3-carboxylic acid (S-1255). 1. Study on structure-activity relationships and bas
J Med Chem 45: 2041-55 (2002)
Shionogi
Structure-based design of a parallel synthetic array directed toward the discovery of irreversible inhibitors of human rhinovirus 3C protease.
J Med Chem 45: 2016-23 (2002)
Pfizer
Synthesis, in vitro receptor binding, and in vivo evaluation of fluorescein and carbocyanine peptide-based optical contrast agents.
J Med Chem 45: 2003-15 (2002)
Washington University
Solid-phase library synthesis, screening, and selection of tight-binding reduced peptide bond inhibitors of a recombinant Leishmania mexicana cysteine protease B.
J Med Chem 45: 1971-82 (2002)
Carlsberg Laboratory
Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines.
J Med Chem 45: 1963-6 (2002)
Glaxosmithkline
Nanomolar inhibitors of Staphylococcus aureus methionyl tRNA synthetase with potent antibacterial activity against gram-positive pathogens.
J Med Chem 45: 1959-62 (2002)
TBA
Pyrazolo[3,4-b]quinoxalines. A new class of cyclin-dependent kinases inhibitors.
Bioorg Med Chem 10: 2177-84 (2002)
Universidad De Navarra
Aminoglycosides modified by resistance enzymes display diminished binding to the bacterial ribosomal aminoacyl-tRNA site.
Chem Biol 9: 455-63 (2002)
Wayne State University
Haploscleridamine, a novel tryptamine-derived alkaloid from a sponge of the order haplosclerida: an inhibitor of cathepsin K.
J Nat Prod 65: 628-9 (2002)
Millennium Pharmaceuticals
A new dimeric dihydrochalcone and a new prenylated flavone from the bud covers of Artocarpus altilis: potent inhibitors of cathepsin K.
J Nat Prod 65: 624-7 (2002)
Millennium Pharmaceuticals
Two new furanoditerpenes from Saururus chinenesis and their effects on the activation of peroxisome proliferator-activated receptor gamma.
J Nat Prod 65: 616-7 (2002)
Korea Research Institute Of Bioscience And Biotechnology
Synthesis and structure-activity relationship study of lamellarin derivatives.
J Nat Prod 65: 500-4 (2002)
Nagasaki University
New antiinfective and human 5-HT2 receptor binding natural and semisynthetic compounds from the Jamaican sponge Smenospongia aurea.
J Nat Prod 65: 476-80 (2002)
The University Of Mississippi
Synthesis and biological evaluation of hyperforin analogues. Part I. Modification of the enolized cyclohexanedione moiety.
J Nat Prod 65: 433-8 (2002)
Universit£
Novel diamide-based inhibitors of IMPDH.
Bioorg Med Chem Lett 12: 1323-6 (2002)
Bristol-Myers Squibb Pharmaceutical Research Institute
Enantiospecific, selective cyclooxygenase-2 inhibitors.
Bioorg Med Chem Lett 12: 1315-8 (2002)
Vanderbilt University School Of Medicine
Benzimidazole-based fXa inhibitors with improved thrombin and trypsin selectivity.
Bioorg Med Chem Lett 12: 1311-4 (2002)
Berlex Biosciences
Design and synthesis of aminophenol-based factor Xa inhibitors.
Bioorg Med Chem Lett 12: 1307-10 (2002)
Berlex Biosciences
Optimization of the 4-aryl group of 4-aryl-pyridine glucagon antagonists: development of an efficient, alternative synthesis.
Bioorg Med Chem Lett 12: 1303-6 (2002)
Bayer Research Center
Small ligands interacting with the phosphotyrosine binding pocket of the Src SH2 protein.
Bioorg Med Chem Lett 12: 1295-8 (2002)
Aventis Pharma
Discovery of highly potent Src SH2 binders: structure-activity studies and X-ray structures.
Bioorg Med Chem Lett 12: 1291-4 (2002)
Aventis Pharma
Imidazole-based ligands of the Src SH2 protein.
Bioorg Med Chem Lett 12: 1287-9 (2002)
Aventis Pharma
Synthesis of a novel fluorescent probe for estrogen receptor.
Bioorg Med Chem Lett 12: 1283-5 (2002)
Abbott Laboratories
The mechanism of the irreversible inhibition of estrone sulfatase (ES) through the consideration of a range of methane- and amino-sulfonate-based compounds.
Bioorg Med Chem Lett 12: 1279-82 (2002)
Kingston University
Design, synthesis and biological activity of novel non-peptidyl endothelin converting enzyme inhibitors, 1-phenyl-tetrazole-formazan analogues.
Bioorg Med Chem Lett 12: 1275-8 (2002)
Sumitomo Pharmaceuticals
Potent inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
Bioorg Med Chem Lett 12: 1269-73 (2002)
Merck Research Laboratories
Enantioselective synthesis of S-(+)-2beta-carboalkoxy-3alpha-[bis(4-fluorophenyl)methoxy]tropanes as novel probes for the dopamine transporter.
Bioorg Med Chem Lett 12: 1249-52 (2002)
National Institute On Drug Abuse-Intramural Research Program
Structure-activity relationships for mini atrial natriuretic peptide by proline-scanning mutagenesis and shortening of peptide backbone.
Bioorg Med Chem Lett 12: 1245-7 (2002)
Institute For Bioorganic Research
Synthesis of a molecular mimic of the Glc1Man9 oligoside as potential inhibitor of calnexin binding to DeltaF508 CFTR protein.
Bioorg Med Chem Lett 12: 1237-40 (2002)
Institut Curie
Interaction of morphine, fentanyl, sufentanil, alfentanil, and loperamide with the efflux drug transporter P-glycoprotein.
Anesthesiology 96: 913-20 (2002)
Vanderbilt University
Expression and functional characterization of rat organic anion transporter 3 (rOat3) in the choroid plexus.
Mol Pharmacol 61: 982-8 (2002)
University Of Tokyo
Three-dimensional quantitative structure-activity relationships of inhibitors of P-glycoprotein.
Mol Pharmacol 61: 964-73 (2002)
Eli Lilly
Agonist, antagonist, and inverse agonist characteristics of TIPP (H-Tyr-Tic-Phe-Phe-OH), a selective delta-opioid receptor ligand.
J Pharmacol Exp Ther 301: 661-71 (2002)
University Of Arkansas
Biochemical and behavioral characterization of novel methylphenidate analogs.
J Pharmacol Exp Ther 301: 527-35 (2002)
Mercer University
Studies on the synthesis and opioid agonistic activities of mitragynine-related indole alkaloids: discovery of opioid agonists structurally different from other opioid ligands.
J Med Chem 45: 1949-56 (2002)
Chiba University
Synthesis of N-[4-[1-ethyl-2-(2,4-diaminofuro[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid as an antifolate.
J Med Chem 45: 1942-8 (2002)
Duquesne University
Further studies on conformationally constrained tricyclic tropane analogues and their uptake inhibition at monoamine transporter sites: synthesis of (Z)-9-(substituted arylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes as a novel class of serotonin transporter inhibitors.
J Med Chem 45: 1930-41 (2002)
Georgetown University Medical Center
Synthesis and biological evaluation of structurally highly modified analogues of the antimitotic natural product curacin A.
J Med Chem 45: 1901-17 (2002)
University Of Pittsburgh
3-Heteroaryl-2-pyridones: benzodiazepine site ligands with functional delectivity for alpha 2/alpha 3-subtypes of human GABA(A) receptor-ion channels.
J Med Chem 45: 1887-900 (2002)
Merck Sharp & Dohme Research Laboratories
Halogenated diazirines as photolabel mimics of the inhaled haloalkane anesthetics.
J Med Chem 45: 1879-86 (2002)
University Of Pennsylvania Health System
Synthesis of nitroindole derivatives with high affinity and selectivity for melatoninergic binding sites MT(3).
J Med Chem 45: 1853-9 (2002)
Institut De Chimie Pharmaceutique Albert Lespagnol
5'-Deoxy congeners of 9-(3-amido-3-deoxy-beta-D-xylofuranosyl)-N(6)-cyclopentyladenine: new adenosine A(1) receptor antagonists and inverse agonists.
J Med Chem 45: 1845-52 (2002)
Ghent University
Identification of nonpeptidic urotensin II receptor antagonists by virtual screening based on a pharmacophore model derived from structure-activity relationships and nuclear magnetic resonance studies on urotensin II.
J Med Chem 45: 1799-805 (2002)
Aventis Pharma Germany
Investigation of potential bioisosteric replacements for the carboxyl groups of peptidomimetic inhibitors of protein tyrosine phosphatase 1B: identification of a tetrazole-containing inhibitor with cellular activity.
J Med Chem 45: 1785-98 (2002)
Biovitrum
Binding mode analysis of 3-(4-benzoyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamide: a new synthetic histone deacetylase inhibitor inducing histone hyperacetylation, growth inhibition, and terminal cell differentiation.
J Med Chem 45: 1778-84 (2002)
Sapienza University Of Rome
Vinyl sulfide cyclized analogues of angiotensin II with high affinity and full agonist activity at the AT(1) receptor.
J Med Chem 45: 1767-77 (2002)
Uppsala University
Structure-based design of novel potent nonpeptide thrombin inhibitors.
J Med Chem 45: 1757-66 (2002)
Boehringer Ingelheim Pharma
Exploration of the pharmacophore of 3-alkyl-5-arylimidazolidinediones as new CB(1) cannabinoid receptor ligands and potential antagonists: synthesis, lipophilicity, affinity, and molecular modeling.
J Med Chem 45: 1748-56 (2002)
Universit£
Structure-based design and synthesis of 2-benzylidene-benzofuran-3-ones as flavopiridol mimics.
J Med Chem 45: 1741-7 (2002)
Novartis Pharmaceuticals
Bivalent inhibition of beta-tryptase: distance scan of neighboring subunits by dibasic inhibitors.
Bioorg Med Chem Lett 12: 985-8 (2002)
Institut FüR Biochemie
Benzimidazole-4,7-diones as inhibitors of protozoal (Toxoplasma gondii) purine nucleoside phosphorylase.
Bioorg Med Chem Lett 12: 977-9 (2002)
Universit£
Design, synthesis and bioactivity evaluation of tribactam beta lactamase inhibitors.
Bioorg Med Chem Lett 12: 971-5 (2002)
Lek
Novel N-[1-(1-substituted 4-piperidinylmethyl)-4-piperidinyl]benzamides as potent colonic prokinetic agents.
Bioorg Med Chem Lett 12: 967-70 (2002)
Dainippon Pharmaceutical
Identification of a novel, orally bioavailable histamine H(3) receptor antagonist based on the 4-benzyl-(1H-imidazol-4-yl) template.
Bioorg Med Chem Lett 12: 937-41 (2002)
The Schering Plough Research Institute
Oxal hydroxamic acid derivatives with inhibitory activity against matrix metalloproteinases.
Bioorg Med Chem Lett 12: 933-6 (2002)
University Of Bielefeld
Synthesis and evaluation of pseudopeptide analogues of a specific CXCR4 inhibitor, T140: the insertion of an (E)-alkene dipeptide isostere into the betaII'-turn moiety.
Bioorg Med Chem Lett 12: 923-8 (2002)
Kyoto University
Benzimidazoles and isosteric compounds as potent and selective factor Xa inhibitors.
Bioorg Med Chem Lett 12: 919-22 (2002)
Aventis Pharmaceuticals
Structure-activity study of L-cysteine-based N-type calcium channel blockers: optimization of N- and C-terminal substituents.
Bioorg Med Chem Lett 12: 915-8 (2002)
Minase Research Institute
Hydrophobic modifications at 1-phosphate of inositol 1,4,5-trisphosphate analogues enhance receptor binding.
Bioorg Med Chem Lett 12: 911-3 (2002)
The University Of Tokyo
QSAR study on adenosine kinase inhibition of pyrrolo[2,3-d]pyrimidine nucleoside analogues using the hansch approach.
Bioorg Med Chem Lett 12: 899-902 (2002)
Jadavpur University
Tricyclic isoxazoles are novel inhibitors of the multidrug resistance protein (MRP1).
Bioorg Med Chem Lett 12: 883-6 (2002)
Eli Lilly
Dermorphin and deltorphin heptapeptide analogues: replacement of Phe residue by Dmp greatly improves opioid receptor affinity and selectivity.
Bioorg Med Chem Lett 12: 879-81 (2002)
Tohoku Pharmaceutical University
Imidazo[5,1-f]triazin-4(3H)-ones, a new class of potent PDE 5 inhibitors.
Bioorg Med Chem Lett 12: 865-8 (2002)
Bayer
Synthesis of iodinated 3beta-aryltropanes with selective binding to either the dopamine or serotonin transporters.
Bioorg Med Chem Lett 12: 845-7 (2002)
State University Of New York
Amino acid derived sulfonamide hydroxamates as inhibitors of procollagen C-proteinase. Part 2: Solid-phase optimization of side chains.
Bioorg Med Chem Lett 12: 1233-5 (2002)
Roche Bioscience
A practical synthesis of (S) 3-tert-butoxycarbonylamino-2-oxo-2,3,4,5-tetrahydro-1,5-benzodiazepine-1-acetic acid methyl ester as a conformationally restricted dipeptido-mimetic for caspase-1 (ICE) inhibitors.
Bioorg Med Chem Lett 12: 1225-7 (2002)
Vertex Pharmaceuticals
Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.
Bioorg Med Chem Lett 12: 1219-23 (2002)
Merck Research Laboratories
Non-covalent thrombin inhibitors featuring P(3)-heterocycles with P(1)-monocyclic arginine surrogates.
Bioorg Med Chem Lett 12: 1203-8 (2002)
Corvas International
Anthranilate sulfonamide hydroxamate TACE inhibitors. Part 2: SAR of the acetylenic P1' group.
Bioorg Med Chem Lett 12: 1199-202 (2002)
Wyeth-Ayerst Research
Anthranilate sulfonamide hydroxamate TACE inhibitors. Part 1: Structure-based design of novel acetylenic P1' groups.
Bioorg Med Chem Lett 12: 1195-8 (2002)
Wyeth-Ayerst Research
Synthesis and in vitro evaluation of a novel iodinated resiniferatoxin derivative that is an agonist at the human vanilloid VR1 receptor.
Bioorg Med Chem Lett 12: 1189-92 (2002)
Johnson & Johnson Pharmaceutical Research And Development
Novel bicyclic lactam inhibitors of thrombin: highly potent and selective inhibitors.
Bioorg Med Chem Lett 12: 1181-4 (2002)
Shire Biochem
Novel potent antagonists of human neuropeptide Y Y5 receptor. Part 1: 2-oxobenzothiazolin-3-acetic acid derivatives.
Bioorg Med Chem Lett 12: 1171-5 (2002)
Fujisawa Pharmaceutical
Solid-phase synthesis and pharmacological evaluation of analogues of PhTX-12-A potent and selective nicotinic acetylcholine receptor antagonist.
Bioorg Med Chem Lett 12: 1159-62 (2002)
The Royal Danish School Of Pharmacy
Synthesis and pharmacological evaluation of 6-piperidino- and 6-piperazinoalkyl-2(3H)-benzothiazolones as mixed sigma/5-HT(1A) ligands.
Bioorg Med Chem Lett 12: 1149-52 (2002)
Université
Design and synthesis of lignostilbene-alpha,beta-dioxygenase inhibitors.
Bioorg Med Chem Lett 12: 1139-42 (2002)
Riken
A common mechanism underlying promiscuous inhibitors from virtual and high-throughput screening.
J Med Chem 45: 1712-22 (2002)
Northwestern University
Potent, orally active heterocycle-based combretastatin A-4 analogues: synthesis, structure-activity relationship, pharmacokinetics, and in vivo antitumor activity evaluation.
J Med Chem 45: 1697-711 (2002)
Abbott Laboratories
Synthesis and in vitro antitumor activity of new deaza analogues of the nonpolyglutamatable antifolate N(alpha)-(4-amino-4-deoxypteroyl)-N(delta)-hemiphthaloyl-L-ornithine (PT523).
J Med Chem 45: 1690-6 (2002)
Harvard Medical School
Synthesis and biological characterization of L-N(6)-(1-iminoethyl)lysine 5-tetrazole-amide, a prodrug of a selective iNOS inhibitor.
J Med Chem 45: 1686-9 (2002)
Pfizer
Synthesis of photoreactive phosphatidic acid analogues displaying activatory properties on cyclic AMP-phosphodiesterases. Photoaffinity labeling of an isoform of phosphodiesterase.
J Med Chem 45: 1678-85 (2002)
Inserm U352
Human somatostatin receptor specificity of backbone-cyclic analogues containing novel sulfur building units.
J Med Chem 45: 1665-71 (2002)
Hebrew University
Geometry-affinity relationships of the selective serotonin receptor ligand 9-(aminomethyl)-9,10-dihydroanthracene.
J Med Chem 45: 1656-64 (2002)
Virginia Commonwealth University
Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 6. Structure-activity studies of orally bioavailable, 2-pyridone-containing peptidomimetics.
J Med Chem 45: 1607-23 (2002)
Agouron Pharmaceuticals
Development of new hydrogen-bond descriptors and their application to comparative molecular field analyses.
J Med Chem 45: 1585-97 (2002)
University Of Marburg
GBR compounds and mepyramines as cocaine abuse therapeutics: chemometric studies on selectivity using grid independent descriptors (GRIND).
J Med Chem 45: 1577-84 (2002)
Universit£
Synthesis, biological evaluation, and binding mode of novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles targeted at the HIV-1 reverse transcriptase.
J Med Chem 45: 1567-76 (2002)
Sapienza University Of Rome
Beta-C-mannosides as selectin inhibitors.
J Med Chem 45: 1563-6 (2002)
Wyeth Research
Inhibition of protein-protein association by small molecules: approaches and progress.
J Med Chem 45: 1543-58 (2002)
Pfizer
Insight into binding of calyculin A to protein phosphatase 1: isolation of hemicalyculin a and chemical transformation of calyculin A.
Chem Biol 9: 309-19 (2002)
The University Of Tokyo
Evaluation of 7-hydroxy-flavones as inhibitors of oestrone and oestradiol biosynthesis.
J Enzym Inhib 16: 417-24 (2001)
Cardiff University
Carbonic anhydrase activity modulators: synthesis of inhibitors and activators incorporating 2-substituted-thiazol-4-yl-methyl scaffolds.
J Enzym Inhib 16: 351-8 (2001)
UniversitÀ
P-glycoprotein inhibition by the multidrug resistance-reversing agent MS-209 enhances bioavailability and antitumor efficacy of orally administered paclitaxel.
Cancer Chemother Pharmacol 49: 322-8 (2002)
Nihon Schering K.K.
Beta-carbolines as specific inhibitors of cyclin-dependent kinases.
Bioorg Med Chem Lett 12: 1129-32 (2002)
Institute Of Molecular And Cell Biology
Spirocyclic nonpeptide glycoprotein IIb-IIIa antagonists. Part 3: synthesis and SAR of potent and specific 2,8-diazaspiro[4.5]decanes.
Bioorg Med Chem Lett 12: 1103-7 (2002)
Cor Therapeutics
5-Phosphonomethylquinoxalinediones as competitive NMDA receptor antagonists with a preference for the human 1A/2A, rather than 1A/2B receptor composition.
Bioorg Med Chem Lett 12: 1099-102 (2002)
Novartis Pharma
Sulfide analogues as potent and selective M(2) muscarinic receptor antagonists.
Bioorg Med Chem Lett 12: 1087-91 (2002)
Schering-Plough Research Institute
Benzoindoloquinolines interact with DNA tetraplexes and inhibit telomerase.
Bioorg Med Chem Lett 12: 1071-4 (2002)
National Museum Of Natural History
Design, synthesis and in vitro evaluation of potent, novel, small molecule inhibitors of plasminogen activator inhibitor-1.
Bioorg Med Chem Lett 12: 1063-6 (2002)
Xenova
New aromatase inhibitors. Synthesis and inhibitory activity of pyridinyl-substituted flavanone derivatives.
Bioorg Med Chem Lett 12: 1059-61 (2002)
Upres Ea 1085
Squaric acid derivatives as VLA-4 integrin antagonists.
Bioorg Med Chem Lett 12: 1051-4 (2002)
Celltech R&D
Thalidomide and its analogues as cyclooxygenase inhibitors.
Bioorg Med Chem Lett 12: 1043-6 (2002)
The University Of Tokyo
N-alkylaminoacids and their derivatives interact with melanocortin receptors.
Bioorg Med Chem Lett 12: 1039-42 (2002)
Uppsala University
Reductive amination products containing naphthalene and indole moieties bind to melanocortin receptors.
Bioorg Med Chem Lett 12: 1035-8 (2002)
Uppsala University
Noncovalent tripeptidic thrombin inhibitors incorporating amidrazone, amine and amidine functions at P1.
Bioorg Med Chem Lett 12: 1017-22 (2002)
Life Science R & D, Lgci
Novel potent antagonists of human neuropeptide Y-Y5 receptor. Part 4: tetrahydrodiazabenzazulene derivatives.
Bioorg Med Chem Lett 12: 1009-11 (2002)
Fujisawa Pharmaceutical
Azapeptides as inhibitors of the hepatitis C virus NS3 serine protease.
Bioorg Med Chem Lett 12: 1005-8 (2002)
Schering-Plough Research Institute
Thiophene derivatives: a new series of potent norepinephrine and serotonin reuptake inhibitors.
Bioorg Med Chem Lett 12: 993-5 (2002)
Georgetown University Medical Center
Interaction of human organic anion transporters with various cephalosporin antibiotics.
Eur J Pharmacol 438: 137-42 (2002)
Kyorin University
T-226296: a novel, orally active and selective melanin-concentrating hormone receptor antagonist.
Eur J Pharmacol 438: 129-35 (2002)
Takeda Chemical Industries
Nobiloside, a new neuraminidase inhibitory triterpenoidal saponin from the marine sponge Erylus nobilis.
J Nat Prod 65: 411-3 (2002)
The University Of Tokyo
Cyclotheonamide E4 and E5, new potent tryptase inhibitors from an Ircinia species of sponge.
J Nat Prod 65: 259-61 (2002)
Kirin Brewery
4-(2-Chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]5-methyl-N-(2-propynyl)-1,3-thiazol-2-amine hydrochloride (SSR125543A): a potent and selective corticotrophin-releasing factor(1) receptor antagonist. I. Biochemical and pharmacological characterization.
J Pharmacol Exp Ther 301: 322-32 (2002)
Sanofi Synthelabo
Elucidation of vasoactive intestinal peptide pharmacophore for VPAC(1) receptors in human, rat, and guinea pig.
J Pharmacol Exp Ther 301: 37-50 (2002)
National Institutes Of Health
Novel 5-substituted 2,4-thiazolidinedione and 2,4-oxazolidinedione derivatives as insulin sensitizers with antidiabetic activities.
J Med Chem 45: 1518-34 (2002)
Takeda Chemical Industries
4-(4-cycloalkyl/aryl-oxazol-5-yl)benzenesulfonamides as selective cyclooxygenase-2 inhibitors: enhancement of the selectivity by introduction of a fluorine atom and identification of a potent, highly selective, and orally active COX-2 inhibitor JTE-522(1).
J Med Chem 45: 1511-7 (2002)
Central Pharmaceutical Research Institute
1,8-disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists.
J Med Chem 45: 1500-10 (2002)
University Of Bonn
Toward an optimal joint recognition of the S1' subsites of endothelin converting enzyme-1 (ECE-1), angiotensin converting enzyme (ACE), and neutral endopeptidase (NEP).
J Med Chem 45: 1477-86 (2002)
Cnrs
Carbonic anhydrase inhibitors. A general approach for the preparation of water-soluble sulfonamides incorporating polyamino-polycarboxylate tails and of their metal complexes possessing long-lasting, topical intraocular pressure-lowering properties.
J Med Chem 45: 1466-76 (2002)
Universit£
Modeling of binding modes and inhibition mechanism of some natural ligands of farnesyl transferase using molecular docking.
J Med Chem 45: 1460-5 (2002)
University Of Milan
Molecular interaction of the antagonist N-(piperidin-1-yl)-5-(4-chlorophenyl)-1- (2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide with the CB1 cannabinoid receptor.
J Med Chem 45: 1447-59 (2002)
University Of South Carolina
Molecular dynamics and free energy analyses of cathepsin D-inhibitor interactions: insight into structure-based ligand design.
J Med Chem 45: 1412-9 (2002)
University Of California
Identification of novel cyclooxygenase-2 selective inhibitors using pharmacophore models.
J Med Chem 45: 1402-11 (2002)
Laboratorios Menarini
Toward selective ERbeta agonists for central nervous system disorders: synthesis and characterization of aryl benzthiophenes.
J Med Chem 45: 1399-401 (2002)
Novartis Pharmaceuticals
Design, synthesis, and evaluation of opioid analogues with non-peptidic beta-turn scaffold: enkephalin and endomorphin mimetics.
J Med Chem 45: 1395-8 (2002)
TBA
Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site.
Nat Struct Biol 9: 268-72 (2002)
Boehringer Ingelheim Pharmaceuticals
Kinetic and structural studies on the interaction of cholinesterases with the anti-Alzheimer drug rivastigmine.
Biochemistry 41: 3555-64 (2002)
Weizmann Institute Of Science
Comparative inhibitory effects of different compounds on rat oatpl (slc21a1)- and Oatp2 (Slc21a5)-mediated transport.
Pharm Res 19: 147-53 (2002)
Kitasato University
Characterization of phospholipase C activity at h5-HT2C compared with h5-HT2B receptors: influence of novel ligands upon membrane-bound levels of [3H]phosphatidylinositols.
Naunyn Schmiedebergs Arch Pharmacol 365: 242-52 (2002)
Institut De Recherches Servier
Design and synthesis of a novel and potent series of inhibitors of cytosolic phospholipase A(2) based on a 1,3-disubstituted propan-2-one skeleton.
J Med Chem 45: 1348-62 (2002)
Astrazeneca R&D Charnwood
Development of long-acting dopamine transporter ligands as potential cocaine-abuse therapeutic agents: chiral hydroxyl-containing derivatives of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine and 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine.
J Med Chem 45: 1321-9 (2002)
National Institute Of Diabetes And Digestive And Kidney Diseases
Novel 4-anilinoquinazolines with C-7 basic side chains: design and structure activity relationship of a series of potent, orally active, VEGF receptor tyrosine kinase inhibitors.
J Med Chem 45: 1300-12 (2002)
Astrazeneca
First non-ATP competitive glycogen synthase kinase 3 beta (GSK-3beta) inhibitors: thiadiazolidinones (TDZD) as potential drugs for the treatment of Alzheimer's disease.
J Med Chem 45: 1292-9 (2002)
Instituto De Quimica Medica (Csic)
Carbocyclic dinucleoside polyphosphonates: interaction with HIV reverse transcriptase and antiviral activity.
J Med Chem 45: 1284-91 (2002)
Russian Academy Of Sciences
Substituted diphenyl sulfides as selective serotonin transporter ligands: synthesis and in vitro evaluation.
J Med Chem 45: 1253-8 (2002)
University Of Tours
Development of 2,4-diaminopyrimidines as antimalarials based on inhibition of the S108N and C59R+S108N mutants of dihydrofolate reductase from pyrimethamine-resistant Plasmodium falciparum.
J Med Chem 45: 1244-52 (2002)
National Center For Genetic Engineering And Biotechnology At Thailand
PRO_SELECT: combining structure-based drug design and array-based chemistry for rapid lead discovery. 2. The development of a series of highly potent and selective factor Xa inhibitors.
J Med Chem 45: 1221-32 (2002)
Protherics Molecular Design
Synthesis and biological evaluation of 2-substituted 3beta-tolyltropane derivatives at dopamine, serotonin, and norepinephrine transporters.
J Med Chem 45: 1203-10 (2002)
University Of New Orleans
Ribose-modified nucleosides as ligands for adenosine receptors: synthesis, conformational analysis, and biological evaluation of 1'-C-methyl adenosine analogues.
J Med Chem 45: 1196-202 (2002)
Universit£
3-(1H-Pyrrol-1-yl)-2-oxazolidinones as reversible, highly potent, and selective inhibitors of monoamine oxidase type A.
J Med Chem 45: 1180-3 (2002)
Sapienza University Of Rome
6,7-Dihydro-2-benzothiophen-4(5H)-ones: a novel class of GABA-A alpha5 receptor inverse agonists.
J Med Chem 45: 1176-9 (2002)
Merck Sharp & Dohme Research Laboratories
Serine-threonine protein phosphatase inhibitors: development of potential therapeutic strategies.
J Med Chem 45: 1151-75 (2002)
The University Of Newcastle
Comparison between isopropyl unoprostone and latanoprost by prostaglandin E(2)induction, affinity to prostaglandin transporter, and intraocular metabolism.
Exp Eye Res 74: 41-9 (2002)
Yamanashi Medical University
Characterization of (2S,4R)-1-[5-chloro-1-[(2,4-dimethoxyphenyl)sulfonyl]-3-(2-methoxy-phenyl)-2-oxo-2,3-dihydro-1H-indol-3-yl]-4-hydroxy-N,N-dimethyl-2-pyrrolidine carboxamide (SSR149415), a selective and orally active vasopressin V1b receptor antagonist.
J Pharmacol Exp Ther 300: 1122-30 (2002)
Sanofi-Synthelabo Recherche
A structure/activity relationship study on arvanil, an endocannabinoid and vanilloid hybrid.
J Pharmacol Exp Ther 300: 984-91 (2002)
Istituto Di Chimica Biomolecolare
Functional involvement of rat organic anion transporter 3 (rOat3; Slc22a8) in the renal uptake of organic anions.
J Pharmacol Exp Ther 300: 746-53 (2002)
University Of Tokyo
Structure-activity relationships of oxime neurokinin antagonists: oxime modifications.
Bioorg Med Chem Lett 12: 833-6 (2002)
Schering-Plough Research Institute
2-Arylindoles as gonadotropin releasing hormone (GnRH) antagonists: optimization of the tryptamine side chain.
Bioorg Med Chem Lett 12: 827-32 (2002)
Merck Research Laboratories
Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 2: 4-substituted 6-nitroquipazines.
Bioorg Med Chem Lett 12: 811-5 (2002)
Inha University
Novel potent antagonists of human neuropeptide Y Y5 receptors. Part 3: 7-methoxy-1-hydroxy-1-substituted tetraline derivatives.
Bioorg Med Chem Lett 12: 799-802 (2002)
Fujisawa Pharmaceutical
Synthesis and structure-activity relationships of M(2)-selective muscarinic receptor ligands in the 1-[4-(4-arylsulfonyl)-phenylmethyl]-4-(4-piperidinyl)-piperazine family.
Bioorg Med Chem Lett 12: 795-8 (2002)
Schering-Plough Research Institute
Substituted 2-(R)-methyl piperazines as muscarinic M(2) selective ligands.
Bioorg Med Chem Lett 12: 791-4 (2002)
Schering-Plough Research Institute
Potent nonsteroidal progesterone receptor agonists: synthesis and SAR study of 6-aryl benzoxazines.
Bioorg Med Chem Lett 12: 787-90 (2002)
Wyeth Research
Synthesis and activity of a new methoxytetrahydropyran derivative as dual cyclooxygenase-2/5-lipoxygenase inhibitor.
Bioorg Med Chem Lett 12: 779-82 (2002)
Laboratoires Innothera
Novel agents combining platelet activating factor (PAF) receptor antagonist with thromboxane synthase inhibitor (TxSI).
Bioorg Med Chem Lett 12: 771-4 (2002)
Nikken Chemicals
Novel potent antagonists of human neuropeptide Y Y5 receptors. Part 2: substituted benzo[a]cycloheptene derivatives.
Bioorg Med Chem Lett 12: 757-61 (2002)
Fujisawa Pharmaceutical
Anionic cyclophanes as potential reversal agents of muscle relaxants by chemical chelation.
Bioorg Med Chem Lett 12: 753-5 (2002)
Organon Laboratories
Synthesis of an alpha-fucosidase inhibitor, 5a-carba-beta-L-fucopyranosylamine, and fucose-type alpha- and beta-DL-valienamine unsaturated derivatives.
Bioorg Med Chem Lett 12: 749-52 (2002)
Keio University
Novel, potent non-covalent thrombin inhibitors incorporating p(3)-lactam scaffolds.
Bioorg Med Chem Lett 12: 743-8 (2002)
Corvas International
N-aryl 2,6-dimethoxybiphenylalanine analogues as VLA-4 antagonists.
Bioorg Med Chem Lett 12: 729-31 (2002)
Merck Research Laboratories
New sugar-mimic alkaloids from the pods of Angylocalyx pynaertii.
J Nat Prod 65: 198-202 (2002)
Hokuriku University
Constituents of the bark and twigs of Artocarpus dadah with cyclooxygenase inhibitory activity.
J Nat Prod 65: 163-9 (2002)
University Of Illinois At Chicago
Development of a new class of nonimidazole histamine H(3) receptor ligands with combined inhibitory histamine N-methyltransferase activity.
J Med Chem 45: 1128-41 (2002)
Freie UniversitäT Berlin
Side-chain lactam-bridge conformational constraints differentiate the activities of salmon and human calcitonins and reveal a new design concept for potent calcitonin analogues.
J Med Chem 45: 1108-21 (2002)
Rutgers University
6-Sulfonylchromenes as highly potent K(ATP)-channel openers.
J Med Chem 45: 1086-97 (2002)
Heinrich-Heine-Universit£T
Synthesis and nicotinic binding studies on enantiopure diazine analogues of the novel (2-chloro-5-pyridyl)-9-azabicyclo[4.2.1]non-2-ene UB-165.
J Med Chem 45: 1064-72 (2002)
Institut F£R Pharmazeutische Chemie Der Philipps-Universit£T Marburg
Nanomolar small molecule inhibitors for alphav(beta)6, alphav(beta)5, and alphav(beta)3 integrins.
J Med Chem 45: 1045-51 (2002)
Merck
Synthesis and biological evaluation of a new set of pyrazolo[1,5-c]quinazoline-2-carboxylates as novel excitatory amino acid antagonists.
J Med Chem 45: 1035-44 (2002)
Universita' Di Firenze
Bis(1H-2-indolyl)methanones as a novel class of inhibitors of the platelet-derived growth factor receptor kinase.
J Med Chem 45: 1002-18 (2002)
University Of Regensburg
Identification of novel inhibitors of the transforming growth factor beta1 (TGF-beta1) type 1 receptor (ALK5).
J Med Chem 45: 999-1001 (2002)
Glaxosmithkline
Evolution, synthesis and SAR of tripeptide alpha-ketoacid inhibitors of the hepatitis C virus NS3/NS4A serine protease.
Bioorg Med Chem Lett 12: 705-8 (2002)
Irbm, Mrl Rome
A designed P1 cysteine mimetic for covalent and non-covalent inhibitors of HCV NS3 protease.
Bioorg Med Chem Lett 12: 701-4 (2002)
Irbm, Mrl Rome
Insertion of 2-carboxysuccinate and tricarballylic acid fragments into cyclic-pseudopeptides: new antagonists for the human tachykinin NK-2 receptor.
Bioorg Med Chem Lett 12: 693-6 (2002)
Menarini Ricerche S.P.A. Laboratori Di Firenze
Pyridazine based inhibitors of p38 MAPK.
Bioorg Med Chem Lett 12: 689-92 (2002)
Merck Research Laboratories
Identification of unique VLA-4 antagonists from a combinatorial library.
Bioorg Med Chem Lett 12: 685-8 (2002)
Merck Research Laboratories
CCR5 antagonists: bicyclic isoxazolidines as conformationally constrained N-1-substituted pyrrolidines.
Bioorg Med Chem Lett 12: 677-9 (2002)
Merck Research Laboratories
Human glucagon receptor antagonists based on alkylidene hydrazides.
Bioorg Med Chem Lett 12: 663-6 (2002)
Pfizer
Synthesis and biological evaluation of imidazol-2-one and 2-cyanoiminoimidazole derivatives: novel series of PDE4 inhibitors.
Bioorg Med Chem Lett 12: 653-8 (2002)
Janssen-Cilag
4-amidinobenzylamine-based inhibitors of urokinase.
Bioorg Med Chem Lett 12: 645-8 (2002)
Universitat Jena
Solution and solid-phase synthesis of potent inhibitors of hepatitis C virus NS3 proteinase.
Bioorg Med Chem Lett 12: 641-3 (2002)
Roche Discovery Welwyn
Substituted N-(3,5-dichlorobenzenesulfonyl)-L-prolyl-phenylalanine analogues as potent VLA-4 antagonists.
Bioorg Med Chem Lett 12: 637-40 (2002)
Merck Research Laboratories
Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy.
Bioorg Med Chem Lett 12: 633-6 (2002)
Friedrich-Alexander University
A new class of type I protein geranylgeranyltransferase (GGTase I) inhibitor.
Bioorg Med Chem Lett 12: 629-32 (2002)
Banyu Tsukuba Research Institute
A novel series of hybrid compounds derived by combining 2-aminotetralin and piperazine fragments: binding activity at D2 and D3 receptors.
Bioorg Med Chem Lett 12: 619-22 (2002)
Wayne State University
The discovery of acylated beta-amino acids as potent and orally bioavailable VLA-4 antagonists.
Bioorg Med Chem Lett 12: 611-4 (2002)
Merck Research Laboratories
Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 2.
Bioorg Med Chem Lett 12: 607-10 (2002)
Nippon Roche Research Center
Synthesis of 5,6-dihydro-11H-benzo[5,6]-cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidine-N-cyanoguanidine derivatives as inhibitors of ras farnesyl protein transferase.
Bioorg Med Chem Lett 12: 601-5 (2002)
Schering-Plough Research Institute
Encounter with unexpected collagenase-1 selective inhibitor: switchover of inhibitor binding pocket induced by fluorine atom.
Bioorg Med Chem Lett 12: 581-4 (2002)
Organon K.K.
2-(anilinomethyl)imidazolines as alpha1A adrenergic receptor agonists: 2'-heteroaryl and 2'-oxime ether series.
Bioorg Med Chem Lett 12: 575-9 (2002)
Glaxosmithkline
Studies on quinazolinones as dual inhibitors of Pgp and MRP1 in multidrug resistance.
Bioorg Med Chem Lett 12: 571-4 (2002)
Xenova
Design and synthesis of peptide-based carboxylic acid-containing transition-state inhibitors of human neutrophil elastase.
Bioorg Med Chem Lett 12: 551-5 (2002)
Dainippon Pharmaceutical
Structure-based design of cyclooxygenase-2 selectivity into ketoprofen.
Bioorg Med Chem Lett 12: 533-7 (2002)
Laboratorios Menarini
A combinatorial library of indinavir analogues and its in vitro and in vivo studies.
Bioorg Med Chem Lett 12: 529-32 (2002)
Merck Research Laboratories
Differential inhibition of polymerase and strand-transfer activities of HIV-1 reverse transcriptase.
Bioorg Med Chem Lett 12: 525-8 (2002)
University Of Toledo
Amide derivatives of meclofenamic acid as selective cyclooxygenase-2 inhibitors.
Bioorg Med Chem Lett 12: 521-4 (2002)
Vanderbilt University School Of Medicine
Biphenylsulfonamide endothelin receptor antagonists. Part 3: structure-activity relationship of 4'-heterocyclic biphenylsulfonamides.
Bioorg Med Chem Lett 12: 517-20 (2002)
Bristol-Myers Squibb Pharmaceutical Research Institute
Transport activity of human MRP3 expressed in Sf9 cells: comparative studies with rat MRP3.
Pharm Res 19: 34-41 (2002)
The University Of Tokyo
Selective antagonists at group I metabotropic glutamate receptors: synthesis and molecular pharmacology of 4-aryl-3-isoxazolol amino acids.
J Med Chem 45: 988-91 (2002)
The Royal Danish School Of Pharmacy
Cyclohexylmethylpiperidinyltriphenylpropioamide: a selective muscarinic M(3) antagonist discriminating against the other receptor subtypes.
J Med Chem 45: 984-7 (2002)
Banyu Tsukuba Research Institute
Computational studies on tetrahydropyrimidine-2-one HIV-1 protease inhibitors: improving three-dimensional quantitative structure-activity relationship comparative molecular field analysis models by inclusion of calculated inhibitor- and receptor-based properties.
J Med Chem 45: 973-83 (2002)
University Of Missouri-St. Louis
Novel antagonists acting at the P2Y(1) purinergic receptor: synthesis and conformational analysis using potentiometric and nuclear magnetic resonance titration techniques.
J Med Chem 45: 962-72 (2002)
Universit£
New strategy for antedrug application: development of metalloproteinase inhibitors as antipsoriatic drugs.
J Med Chem 45: 930-6 (2002)
Organon K.K.
New type of metalloproteinase inhibitor: design and synthesis of new phosphonamide-based hydroxamic acids.
J Med Chem 45: 919-29 (2002)
Nippon Organon K.K.
Cysteine derivatives as inhibitors for carboxypeptidase A: synthesis and structure-activity relationships.
J Med Chem 45: 911-8 (2002)
Pohang University Of Science And Technology
Pyridophens: binary pyridostigmine-aprophen prodrugs with differential inhibition of acetylcholinesterase, butyrylcholinesterase, and muscarinic receptors.
J Med Chem 45: 902-10 (2002)
Institute Of Research
Structural aspects of isozyme selectivity in the binding of inhibitors to carbonic anhydrases II and IV.
J Med Chem 45: 888-93 (2002)
University Of Pennsylvania
Structural basis of RasGRP binding to high-affinity PKC ligands.
J Med Chem 45: 853-60 (2002)
Georgetown University Medical Center
CoMFA and CoMSIA 3D QSAR and docking studies on conformationally-restrained cinnamoyl HIV-1 integrase inhibitors: exploration of a binding mode at the active site.
J Med Chem 45: 841-52 (2002)
University Of Tennessee Health Science Center
Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
J Med Chem 45: 789-804 (2002)
Novo Nordisk
Synthesis, biological activity, and molecular modeling investigation of new pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as human A(3) adenosine receptor antagonists.
J Med Chem 45: 770-80 (2002)
Università
Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates.
J Med Chem 45: 753-7 (2002)
TBA
Dynamic deconvolution of a pre-equilibrated dynamic combinatorial library of acetylcholinesterase inhibitors.
Chembiochem 2: 438-44 (2001)
UniversitÉ
Inhibition studies of porphobilinogen synthase from Escherichia coli differentiating between the two recognition sites.
Chembiochem 2: 343-54 (2001)
University Of NeuchÂTel
Localization of organic anion transport protein 2 in the apical region of rat retinal pigment epithelium.
Invest Ophthalmol Vis Sci 43: 510-4 (2002)
University Hospital
Complexation and chiral recognition thermodynamics of 6-amino-6-deoxy-beta-cyclodextrin with anionic, cationic, and neutral chiral guests: counterbalance between van der Waals and coulombic interactions.
J Am Chem Soc 124: 813-26 (2002)
Japan Science And Technology Agency
Uraemic toxins induce proximal tubular injury via organic anion transporter 1-mediated uptake.
Br J Pharmacol 135: 555-63 (2002)
Tokyo Women'S Medical University
7-Methoxyfuro[2,3-c]pyridine-4-carboxamides as PDE4 inhibitors: a potential treatment for asthma.
Bioorg Med Chem Lett 12: 509-12 (2002)
Celltech R&D
N-arylalkylpiperidines as high-affinity sigma-1 and sigma-2 receptor ligands: phenylpropylamines as potential leads for selective sigma-2 agents.
Bioorg Med Chem Lett 12: 497-500 (2002)
University Of Maryland
Design and synthesis of 4,5-disubstituted-thiophene-2-amidines as potent urokinase inhibitors.
Bioorg Med Chem Lett 12: 491-5 (2002)
3-Dimensional Pharmaceuticals
alpha(1)-Adrenoceptor agonists: the identification of novel alpha(1A )subtype selective 2'-heteroaryl-2-(phenoxymethyl)imidazolines.
Bioorg Med Chem Lett 12: 471-5 (2002)
Glaxosmithkline
Synthesis and biological evaluation of 2-indolyloxazolines as a new class of tubulin polymerization inhibitors. Discovery of A-289099 as an orally active antitumor agent.
Bioorg Med Chem Lett 12: 465-9 (2002)
Abbott Laboratories
Discovery of 5-hydroxyalkyl-4-phenylpyridines as a new class of glucagon receptor antagonists.
Bioorg Med Chem Lett 12: 461-4 (2002)
Bayer Research Center
Synthesis of an alpha-aminophosphonate nucleoside as an inhibitor of S-adenosyl-L-homocysteine hydrolase.
Bioorg Med Chem Lett 12: 457-60 (2002)
University Of Waterloo
Synthesis and SAR of N-substituted dibenzazepinone derivatives as novel potent and selective alpha(V)beta(3) antagonists.
Bioorg Med Chem Lett 12: 441-6 (2002)
Knoll
alpha(1)-Adrenoceptor antagonists. Rational design, synthesis and biological evaluation of new trazodone-like compounds.
Bioorg Med Chem Lett 12: 437-40 (2002)
Universit£
4-Anilino-3-cyanobenzo[g]quinolines as kinase inhibitors.
Bioorg Med Chem Lett 12: 423-5 (2002)
Wyeth-Ayerst Research
[(3)H]-M-MPEP, a potent, subtype-selective radioligand for the metabotropic glutamate receptor subtype 5.
Bioorg Med Chem Lett 12: 407-9 (2002)
Novartis Pharma
A novel synthesis of 2-arylpyrrolo[1,2-a]pyrimid-7-ones and their structure-activity relationships as potent GnRH receptor antagonists.
Bioorg Med Chem Lett 12: 403-6 (2002)
Neurocrine Biosciences
Initial structure-activity relationship studies of a novel series of pyrrolo[1,2-a]pyrimid-7-ones as GnRH receptor antagonists.
Bioorg Med Chem Lett 12: 399-402 (2002)
Neurocrine Biosciences
The first two cantharidin analogues displaying PP1 selectivity.
Bioorg Med Chem Lett 12: 391-3 (2002)
The University Of Newcastle
Dihydropyridine neuropeptide Y Y(1) receptor antagonists.
Bioorg Med Chem Lett 12: 379-82 (2002)
Pharmaceutical Research Institute
Design and synthesis of dual inhibitors for matrix metalloproteinase and cathepsin.
Bioorg Med Chem Lett 12: 375-8 (2002)
Organon K.K.
2-Amino-4-[3'-hydroxyphenyl]-4-hydroxybutanoic acid; a potent inhibitor of rat and recombinant human kynureninase.
Bioorg Med Chem Lett 12: 361-3 (2002)
University Of St. Andrews
Approach to dual-acting platelet activating factor (PAF) receptor antagonist/thromboxane synthase inhibitor (TxSI) based on the link of PAF antagonists and TxSIs.
Bioorg Med Chem Lett 12: 341-4 (2002)
Nikken Chemicals
Novel dihydropyrazine analogues as NPY antagonists.
Bioorg Med Chem Lett 12: 337-40 (2002)
Bristol-Myers Squibb Pharmaceutical Research Institute
Enantio-dependent binding and transactivation of optically active phenylpropanoic acid derivatives at human peroxisome proliferator-activated receptor alpha.
Bioorg Med Chem Lett 12: 333-5 (2002)
Kyorin Pharmaceutical
Tyrosylprotein sulfotransferase inhibitors generated by combinatorial target-guided ligand assembly.
Bioorg Med Chem Lett 12: 329-32 (2002)
University Of California
Discovery of a nonpeptidic small molecule antagonist of the human platelet thrombin receptor (PAR-1).
Bioorg Med Chem Lett 12: 319-23 (2002)
Merck Research Laboratories
Studies toward the discovery of the next generation of antidepressants. Part 2: incorporating a 5-HT(1A) antagonist component into a class of serotonin reuptake inhibitors.
Bioorg Med Chem Lett 12: 307-10 (2002)
Wyeth-Ayerst Research Laboratories
Synthesis and evaluation of imidazo[1,5-a]pyrazines as corticotropin releasing hormone receptor ligands.
Bioorg Med Chem Lett 12: 291-4 (2002)
Dupont Pharmaceuticals
Biotinylated lithocholic acids for affinity chromatography of mammalian DNA polymerases alpha and beta.
Bioorg Med Chem Lett 12: 287-90 (2002)
Tokyo University Of Science
New generation dopaminergic agents. Part 8: heterocyclic bioisosteres that exploit the 7-OH-2-(aminomethyl)chroman D(2) template.
Bioorg Med Chem Lett 12: 271-4 (2002)
Wyeth-Ayerst Research Laboratories
Estimation of binding affinities for celecoxib analogues with COX-2 via Monte Carlo-extended linear response.
Bioorg Med Chem Lett 12: 267-70 (2002)
Yale University
A(3) adenosine receptors in human neutrophils and promyelocytic HL60 cells: a pharmacological and biochemical study.
Mol Pharmacol 61: 415-24 (2002)
University Of Ferrara
Binding characteristics of cetirizine and levocetirizine to human H(1) histamine receptors: contribution of Lys(191) and Thr(194).
Mol Pharmacol 61: 391-9 (2002)
Ucb Pharma
A prolyl endopeptidase-inhibiting benzofuran dimer from Polyozellus multiflex.
J Nat Prod 65: 76-8 (2002)
Kyungpook National University
New chlorinated diphenyl ethers from an Aspergillus species.
J Nat Prod 65: 7-10 (2002)
University Of Western Australia
Evaluation of the Dmt-Tic pharmacophore: conversion of a potent delta-opioid receptor antagonist into a potent delta agonist and ligands with mixed properties.
J Med Chem 45: 713-20 (2002)
University Of Cagliary
Novel mycophenolic adenine bis(phosphonate) analogues as potential differentiation agents against human leukemia.
J Med Chem 45: 703-12 (2002)
Pharmasset
Synthesis of 1-(3,4-dihydroxy-5-nitrophenyl)-2-phenyl-ethanone and derivatives as potent and long-acting peripheral inhibitors of catechol-O-methyltransferase.
J Med Chem 45: 685-95 (2002)
Department Of Research & Development
Identification of potent and selective mechanism-based inhibitors of the cysteine protease cruzain using solid-phase parallel synthesis.
J Med Chem 45: 676-84 (2002)
University Of California
Design and synthesis of motilin antagonists derived from the [1-4] fragment of porcine motilin.
J Med Chem 45: 670-5 (2002)
Chugai Pharmaceutical
Expansion of structure-activity studies of piperidine analogues of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine (GBR 12935) compounds by altering substitutions in the N-benzyl moiety and behavioral pharmacology of selected molecules.
J Med Chem 45: 654-62 (2002)
Wayne State University
Synthesis and optimization of a new family of type 3 17 beta-hydroxysteroid dehydrogenase inhibitors by parallel liquid-phase chemistry.
J Med Chem 45: 640-53 (2002)
Centre Hospitalier Universitaire De Qu£Bec And Universit£
Synthesis and preliminary characterization of a novel antiarrhythmic compound (KB130015) with an improved toxicity profile compared with amiodarone.
J Med Chem 45: 623-30 (2002)
Karo Bio
Antitumor polycyclic acridines. 8.(1) Synthesis and telomerase-inhibitory activity of methylated pentacyclic acridinium salts.
J Med Chem 45: 590-7 (2002)
University Of Nottingham
Synthesis and evaluation of potent and selective beta(3) adrenergic receptor agonists containing acylsulfonamide, sulfonylsulfonamide, and sulfonylurea carboxylic acid isosteres.
J Med Chem 45: 567-83 (2002)
Glaxosmithkline
Discovery of a 3-amino-6-phenyl-pyridazine derivative as a new synthetic antineuroinflammatory compound.
J Med Chem 45: 563-6 (2002)
TBA
Designing non-peptide peptidomimetics in the 21st century: inhibitors targeting conformational ensembles.
J Med Chem 45: 541-58 (2002)
University Of Wisconsin-Madison
Preclinical pharmacology of fiduxosin, a novel alpha(1)-adrenoceptor antagonist with uroselective properties.
J Pharmacol Exp Ther 300: 478-86 (2002)
Abbott Laboratories
Effect of 17 beta-estradiol-D-17 beta-glucuronide on the rat organic anion transporting polypeptide 2-mediated transport differs depending on substrates.
Drug Metab Dispos 30: 220-3 (2002)
The University Of Tokyo
4'-Arylpyrrolomorphinans: effect of a pyrrolo-N-benzyl substituent in enhancing delta-opioid antagonist activity.
J Med Chem 45: 537-40 (2002)
University Of Bristol
Design, synthesis, and pharmacological evaluation of new farnesyl protein transferase inhibitors.
J Med Chem 45: 533-6 (2002)
Universit£
Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1).
J Med Chem 45: 529-32 (2002)
University Of Utah
Orally-effective, long-acting sorbitol dehydrogenase inhibitors: synthesis, structure-activity relationships, and in vivo evaluations of novel heterocycle-substituted piperazino-pyrimidines.
J Med Chem 45: 511-28 (2002)
Pfizer
4-(Phenylsulfonyl)piperidines: novel, selective, and bioavailable 5-HT(2A) receptor antagonists.
J Med Chem 45: 492-503 (2002)
Merck Sharp And Dohme Research Laboratories
Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1.
J Med Chem 45: 438-48 (2002)
Pharmazeutisches Institut Der UniversitäT Freiburg
2,5'-Disubstituted adenosine derivatives: evaluation of selectivity and efficacy for the adenosine A(1), A(2A), and A(3) receptor.
J Med Chem 45: 420-9 (2002)
Leiden/Amsterdam Center For Drug Research
C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump.
J Med Chem 45: 390-8 (2002)
Georgetown University School Of Medicine
Beta-strand mimicking macrocyclic amino acids: templates for protease inhibitors with antiviral activity.
J Med Chem 45: 371-81 (2002)
University Of Queensland
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
J Med Chem 45: 344-59 (2002)
Universit£
Elucidating the inhibiting mode of AHPBA derivatives against HIV-1 protease and building predictive 3D-QSAR models.
J Med Chem 45: 333-43 (2002)
Chinese Academy Of Sciences
Carbonic anhydrase inhibitors: anticonvulsant sulfonamides incorporating valproyl and other lipophilic moieties.
J Med Chem 45: 312-20 (2002)
University Of Namur
Inhibition of nNOS activity in rat brain by synthetic kynurenines: structure-activity dependence.
J Med Chem 45: 263-74 (2002)
Universidad De Granada
Design of substrate-based inhibitors of human beta-secretase.
J Med Chem 45: 259-62 (2002)
TBA
Stable expression of a synthetic gene for the human motilin receptor: use in an aequorin-based receptor activation assay.
Anal Biochem 300: 146-51 (2002)
Kosan Biosciences
Interaction of omeprazole, lansoprazole and pantoprazole with P-glycoprotein.
Naunyn Schmiedebergs Arch Pharmacol 364: 551-7 (2001)
Institute Of Clinical Pharmacology
Distinct characteristics of organic cation transporters, OCT1 and OCT2, in the basolateral membrane of renal tubules.
Pharm Res 18: 1528-34 (2001)
Kyoto University Hospital
Drug design with a new transition state analog of the hydrated carbonyl: silicon-based inhibitors of the HIV protease.
Chem Biol 8: 1161-6 (2001)
State University Of New York
First dual NK(1) antagonists-serotonin reuptake inhibitors: synthesis and SAR of a new class of potential antidepressants.
Bioorg Med Chem Lett 12: 261-4 (2001)
Ucb Pharma
Cyclic acid anhydrides as a new class of potent, selective and non-peptidic inhibitors of geranylgeranyl transferase.
Bioorg Med Chem Lett 12: 255-9 (2001)
University College London
Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 2.
Bioorg Med Chem Lett 12: 249-53 (2001)
Janssen-Cilag
Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 1.
Bioorg Med Chem Lett 12: 243-8 (2001)
Janssen-Cilag
Synthesis of 4-(8-benzo[1,2,5]oxadiazol-5-yl-[1,7]naphthyridine-6-yl)-benzoic acid: a potent and selective phosphodiesterase type 4D inhibitor.
Bioorg Med Chem Lett 12: 233-5 (2001)
Novartis Pharma
N-Methylbenzanilide derivatives as a novel class of selective V(1A) receptor antagonists.
Bioorg Med Chem Lett 12: 229-32 (2001)
Yamanouchi Pharmaceutical
Synthesis and biological activities of YkFA analogues: effects of position 4 substitutions and altered ring size on in vitro opioid activity.
Bioorg Med Chem Lett 12: 213-6 (2001)
University Of Louisville
Biphenyls as potent vitronectin receptor antagonists.
Bioorg Med Chem Lett 12: 205-8 (2001)
Bayer
3-Aryl pyridone derivatives. Potent and selective kappa opioid receptor agonists.
Bioorg Med Chem Lett 12: 197-200 (2001)
Astrazeneca R&D MöLndal
Oxyaniliniums as acetylcholinesterase inhibitors for the reversal of neuromuscular block.
Bioorg Med Chem Lett 12: 193-6 (2001)
Organon Laboratories
Synthesis and pharmacology of isoquinuclidine derivatives as 5-HT(3) ligands.
Bioorg Med Chem Lett 12: 189-92 (2001)
Universidad De Alcal£
Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 2: (3-Substituted-5-halo-2-pyridinyl)guanidines.
Bioorg Med Chem Lett 12: 185-7 (2001)
Pfizer
Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 1: 2-Pyridinylguanidines.
Bioorg Med Chem Lett 12: 181-4 (2001)
Pfizer
Synthesis and biological activity of 8beta-substituted hydrocodone indole and hydromorphone indole derivatives.
Bioorg Med Chem Lett 12: 165-8 (2001)
Niddk
The discovery of small molecule carbamates as potent dual alpha(4)beta(1)/alpha(4)beta(7) integrin antagonists.
Bioorg Med Chem Lett 12: 159-63 (2001)
Merck Research Laboratories
Evaluation of isotryptamine derivatives at 5-HT(2) serotonin receptors.
Bioorg Med Chem Lett 12: 155-8 (2001)
Virginia Commonwealth University
Mixed lineage kinase activity of indolocarbazole analogues.
Bioorg Med Chem Lett 12: 147-50 (2001)
Kyowa Hakko Kogyo
Synthesis and structure-activity relationships of oxime neurokinin antagonists: discovery of potent arylamides.
Bioorg Med Chem Lett 12: 141-5 (2001)
Schering-Plough Research Institute
N-acyl-L-phenylalanine derivatives as potent VLA-4 antagonists that mimic a cyclic peptide conformation.
Bioorg Med Chem Lett 12: 137-40 (2001)
Hoffmann-La Roche
Specific and dual antagonists of alpha(4)beta(1) and alpha(4)beta(7) integrins.
Bioorg Med Chem Lett 12: 133-6 (2001)
Merck Research Laboratories
The design and synthesis of a novel series of indole derived selective ET(A) antagonists.
Bioorg Med Chem Lett 12: 125-8 (2001)
Pfizer
Effects of the incorporation of IBTM beta-turn mimetics into the dipeptoid CCK(1) receptor agonist PD 170292.
Bioorg Med Chem Lett 12: 109-12 (2001)
Instituto De QuíMica MéDica (Csic)
Screening of triterpenoids isolated from Phyllanthus flexuosus for DNA topoisomerase inhibitory activity.
J Nat Prod 64: 1545-7 (2001)
Osaka University Of Pharmaceutical Sciences
Inhibition of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium dihydrofolate reductases by 2,4-diamino-5-[2-methoxy-5-(omega-carboxyalkyloxy)benzyl]pyrimidines: marked improvement in potency relative to trimethoprim and species selectivity relative to piritrexim.
J Med Chem 45: 233-41 (2001)
Harvard Medical School
Phenoxyphenyl sulfone N-formylhydroxylamines (retrohydroxamates) as potent, selective, orally bioavailable matrix metalloproteinase inhibitors.
J Med Chem 45: 219-32 (2001)
Abbott Laboratories
Methanocarba modification of uracil and adenine nucleotides: high potency of Northern ring conformation at P2Y1, P2Y2, P2Y4, and P2Y11 but not P2Y6 receptors.
J Med Chem 45: 208-18 (2001)
National Institute Of Diabetes
Design and synthesis of potent nonpeptidic farnesyltransferase inhibitors based on a terphenyl scaffold.
J Med Chem 45: 177-88 (2001)
Yale University
Improvement in the selectivity and metabolic stability of the serotonin 5-HT(1A) ligand, S 15535: a series of cis- and trans-2-(arylcycloalkylamine) 1-indanols.
J Med Chem 45: 165-76 (2002)
Institut De Recherches Servier
Design, synthesis, and discovery of novel trans-stilbene analogues as potent and selective human cytochrome P450 1B1 inhibitors.
J Med Chem 45: 160-4 (2001)
Seoul National University
7-Substituted 5-amino-2-(2-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as A2A adenosine receptor antagonists: a study on the importance of modifications at the side chain on the activity and solubility.
J Med Chem 45: 115-26 (2001)
Università
Structure-based design and characterization of novel platforms for ricin and shiga toxin inhibition.
J Med Chem 45: 90-8 (2001)
University Of Texas
Pharmacophore mapping of a series of 2,4-diamino-5-deazapteridine inhibitors of Mycobacterium avium complex dihydrofolate reductase.
J Med Chem 45: 41-53 (2001)
Lindsley F. Kimball Research Institute
Alpha2-adrenoreceptors profile modulation and high antinociceptive activity of (S)-(-)-2-[1-(biphenyl-2-yloxy)ethyl]-4,5-dihydro-1H-imidazole.
J Med Chem 45: 32-40 (2002)
Universit£
Novel 1-hydroxyazole bioisosteres of glutamic acid. Synthesis, protolytic properties, and pharmacology.
J Med Chem 45: 19-31 (2001)
The Royal Danish School Of Pharmacy
Design and synthesis of pyrrolidine-5,5-trans-lactams (5-oxohexahydropyrrolo[3,2-b]pyrroles) as novel mechanism-based inhibitors of human cytomegalovirus protease. 2. Potency and chirality.
J Med Chem 45: 1-18 (2001)
Glaxosmithkline
Nonpeptide tachykinin receptor antagonists. III. SB 235375, a low central nervous system-penetrant, potent and selective neurokinin-3 receptor antagonist, inhibits citric acid-induced cough and airways hyper-reactivity in guinea pigs.
J Pharmacol Exp Ther 300: 314-23 (2002)
Glaxosmithkline
The effects of deleting the mouse neurotensin receptor NTR1 on central and peripheral responses to neurotensin.
J Pharmacol Exp Ther 300: 305-13 (2002)
Merck Research Laboratories
Interaction of common azole antifungals with P glycoprotein.
Antimicrob Agents Chemother 46: 160-5 (2001)
Schering-Plough Research Institute
Extended radioligand binding profile of iloperidone: a broad spectrum dopamine/serotonin/norepinephrine receptor antagonist for the management of psychotic disorders.
Neuropsychopharmacology 25: 904-14 (2001)
Novartis Pharma
Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors.
Neuropsychopharmacology 25: 871-80 (2001)
Eli Lilly
Quantitative distinctions of active site molecular recognition by P-glycoprotein and cytochrome P450 3A4.
Chem Res Toxicol 14: 1596-603 (2001)
Schering-Plough Research Institute
Synthesis of new carboxylesterase inhibitors and evaluation of potency and water solubility.
Chem Res Toxicol 14: 1563-72 (2001)
University Of California At Davis
Synthesis of alkenyldiarylmethane (ADAM) non-nucleoside HIV-1 reverse transcriptase inhibitors with non-identical aromatic rings.
Bioorg Med Chem 10: 283-90 (2002)
Purdue University
Design and synthesis of non-peptidic inhibitors for the Syk C-terminal SH2 domain based on structure-based in-silico screening.
J Med Chem 44: 4737-40 (2001)
Waseda University
Synthesis, in vitro pharmacology, and molecular modeling of syn-huprines as acetylcholinesterase inhibitors.
J Med Chem 44: 4733-6 (2001)
Universitat De Barcelona
Dopamine D(3) receptor antagonists. 1. Synthesis and structure-activity relationships of 5,6-dimethoxy-N-alkyl- and N-alkylaryl-substituted 2-aminoindans.
J Med Chem 44: 4716-32 (2001)
Pharmacia
2-(2-Piperidyl)- and 2-(2-pyrrolidyl)chromans as nicotine agonists: synthesis and preliminary pharmacological characterization.
J Med Chem 44: 4704-15 (2001)
University Of Minnesota
Diaminoindanes as microsomal triglyceride transfer protein inhibitors.
J Med Chem 44: 4677-87 (2001)
Novartis Institute For Biomedical Reasearch
A novel approach for the development of selective Cdk4 inhibitors: library design based on locations of Cdk4 specific amino acid residues.
J Med Chem 44: 4628-40 (2001)
Banyu Tsukuba Research Institute
Structure-based generation of a new class of potent Cdk4 inhibitors: new de novo design strategy and library design.
J Med Chem 44: 4615-27 (2001)
Banyu Tsukuba Research Institute
Structure of protein tyrosine phosphatase 1B in complex with inhibitors bearing two phosphotyrosine mimetics.
J Med Chem 44: 4584-94 (2001)
University Of Waterloo
Design, synthesis, and biological characterization of bivalent 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as selective muscarinic agonists.
J Med Chem 44: 4563-76 (2001)
The University Of Toledo
Synthetic 2-aroylindole derivatives as a new class of potent tubulin-inhibitory, antimitotic agents.
J Med Chem 44: 4535-53 (2001)
University Of Regensburg
Identification of dipeptidyl nitriles as potent and selective inhibitors of cathepsin B through structure-based drug design.
J Med Chem 44: 4524-34 (2001)
Novartis Pharmaceuticals
Quadruplex-interactive agents as telomerase inhibitors: synthesis of porphyrins and structure-activity relationship for the inhibition of telomerase.
J Med Chem 44: 4509-23 (2001)
University Of Texas At Austin
Design, synthesis and biological evaluation of novel arachidonic acid derivatives as highly potent and selective endocannabinoid transporter inhibitors.
J Med Chem 44: 4505-8 (2001)
Universidad Complutense
Characterization of the 1H-cyclopentapyrimidine-2,4(1H,3H)-dione derivative (S)-CPW399 as a novel, potent, and subtype-selective AMPA receptor full agonist with partial desensitization properties.
J Med Chem 44: 4501-4 (2001)
Universita' Degli Studi Di Siena
Synthesis and biological evaluation of myoseverin derivatives: microtubule assembly inhibitors.
J Med Chem 44: 4497-500 (2001)
New York University
Structure-based design of nonpeptide inhibitors of interleukin-1beta converting enzyme (ICE, caspase-1).
Bioorg Med Chem 10: 31-40 (2002)
Pfizer
Potent P1' biphenylmethyl substituted aggrecanase inhibitors.
Bioorg Med Chem Lett 12: 101-4 (2001)
Bristol-Myers Squibb Pharma
Modifications and structure-activity relationships at the 2-position of 4-sulfonamidopyrimidine derivatives as potent endothelin antagonists.
Bioorg Med Chem Lett 12: 81-4 (2001)
Tanabe Seiyaku
Design, synthesis and evaluation of substituted phenylpropanoic acid derivatives as peroxisome proliferator-activated receptor (PPAR) activators: novel human PPARalpha-selective activators.
Bioorg Med Chem Lett 12: 77-80 (2001)
Kyorin Pharmaceutical
4-Aryl/cycloalkyl-5-phenyloxazole derivatives as selective COX-2 inhibitors.
Bioorg Med Chem Lett 12: 65-8 (2001)
Central Pharmaceutical Research Institute
Potent, orally active inhibitors of lipoprotein-associated phospholipase A(2): 1-(biphenylmethylamidoalkyl)-pyrimidones.
Bioorg Med Chem Lett 12: 51-5 (2001)
Glaxosmithkline
Molecular design and structure--activity relationships leading to the potent, selective, and orally active thrombin active site inhibitor BMS-189664.
Bioorg Med Chem Lett 12: 45-9 (2001)
Bristol-Myers Squibb Pharmaceutical Research Institute
Thrombin active site inhibitors: chemical synthesis, in vitro and in vivo pharmacological profile of a novel and selective agent BMS-189090 and analogues.
Bioorg Med Chem Lett 12: 41-4 (2001)
Bristol-Myers Squibb Pharmaceutical Research Institute
Non-peptide alpha(v)beta(3) antagonists. Part 3: identification of potent RGD mimetics incorporating novel beta-amino acids as aspartic acid replacements.
Bioorg Med Chem Lett 12: 31-4 (2001)
Merck Research Laboratories
Nonpeptide alpha(v)beta(3) antagonists. Part 2: constrained glycyl amides derived from the RGD tripeptide.
Bioorg Med Chem Lett 12: 25-9 (2001)
Merck Research Laboratories
Synthesis and biological evaluation of novel thio-substituted chromanes as high-affinity partial agonists for the estrogen receptor.
Bioorg Med Chem Lett 12: 17-9 (2002)
Novo Nordisk
Phthalazine PDE4 inhibitors. Part 3: the synthesis and in vitro evaluation of derivatives with a hydrogen bond acceptor.
Bioorg Med Chem Lett 12: 5-8 (2002)
Zambon Group
Engineering inhibitors highly selective for the S1 sites of Ser190 trypsin-like serine protease drug targets.
Chem Biol 8: 1107-21 (2001)
Axys Pharmaceutical
Nonsteroidal selective glucocorticoid modulators: the effect of C-5 alkyl substitution on the transcriptional activation/repression profile of 2,5-dihydro-10-methoxy-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.
J Med Chem 44: 4481-91 (2001)
Abbott Laboratories
Synthesis and biological studies of novel nucleoside phosphoramidate prodrugs.
J Med Chem 44: 4475-80 (2001)
Purdue University
Novel tropane-based irreversible ligands for the dopamine transporter.
J Med Chem 44: 4453-61 (2001)
National Institute On Drug Abuse-Intramural Research Program
trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT(1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1-arylpiperazines.
J Med Chem 44: 4431-42 (2001)
Università
Synthesis and structure-activity relationships of N-(1-benzylpiperidin-4-yl)arylacetamide analogues as potent sigma1 receptor ligands.
J Med Chem 44: 4404-15 (2001)
Wake Forest University School Of Medicine
Discovery of novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intercellular adhesion molecule-1 interaction. 4. Structure-activity relationship of substituents on the benzene ring of the cinnamide.
J Med Chem 44: 4393-403 (2001)
Abbott Laboratories
Systematic structure-based design and stereoselective synthesis of novel multisubstituted cyclopentane derivatives with potent antiinfluenza activity.
J Med Chem 44: 4379-92 (2001)
Biocryst Pharmaceuticals
[1,2,4]Triazino[4,3-a]benzimidazole acetic acid derivatives: a new class of selective aldose reductase inhibitors.
J Med Chem 44: 4359-69 (2001)
Università
Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): design, synthesis, enzymatic activities, and X-ray crystallographic analysis.
J Med Chem 44: 4339-58 (2001)
Glaxosmithkline
Discovery of small-molecule inhibitors of Bcl-2 through structure-based computer screening.
J Med Chem 44: 4313-24 (2001)
Georgetown University Medical Center
Conformationally constrained analogues of diacylglycerol. 18. The incorporation of a hydroxamate moiety into diacylglycerol-lactones reduces lipophilicity and helps discriminate between sn-1 and sn-2 binding modes to protein kinase C (PK-C). Implications for isozyme specificity.
J Med Chem 44: 4309-12 (2001)
Seoul National University
Design, synthesis and preliminary evaluation of novel 3'-substituted carboxycyclopropylglycines as antagonists at group 2 metabotropic glutamate receptors.
Bioorg Med Chem Lett 11: 3179-82 (2001)
Universit£
Synthesis and HIV-1 integrase inhibitory activities of catechol and bis-catechol derivatives.
Bioorg Med Chem Lett 11: 3175-8 (2001)
Université
[3-cis-3,5-Dimethyl-(1-piperazinyl)alkyl]-bis-(4'-fluorophenyl)amine analogues as novel probes for the dopamine transporter.
Bioorg Med Chem Lett 11: 3169-73 (2001)
National Institute On Drug Abuse-Intramural Research Program
1-Alkyl-3-amino-5-aryl-1H-[1,2,4]triazoles: novel synthesis via cyclization of N-acyl-S-methylisothioureas with alkylhydrazines and their potent corticotropin-releasing factor-1 (CRF(1)) receptor antagonist activities.
Bioorg Med Chem Lett 11: 3165-8 (2001)
Neurocrine Biosciences
Novel bicyclic lactam inhibitors of thrombin: potency and selectivity optimization through P1 residues.
Bioorg Med Chem Lett 11: 3161-4 (2001)
Shire Biochem
Solution-phase, parallel synthesis and pharmacological evaluation of acylguanidine derivatives as potential sodium channel blockers.
Bioorg Med Chem Lett 11: 3151-5 (2001)
Cenes Pharmaceuticals
Discovery, total synthesis, HRV 3C-protease inhibitory activity, and structure-activity relationships of 2-methoxystypandrone and its analogues.
Bioorg Med Chem Lett 11: 3143-6 (2001)
Merck Research Laboratories
Combinatorial synthesis of CCR5 antagonists.
Bioorg Med Chem Lett 11: 3137-41 (2001)
Merck Research Laboratories
Modelling studies of the active site of human sorbitol dehydrogenase: an approach to structure-based inhibitor design of the enzyme.
Bioorg Med Chem Lett 11: 3133-6 (2001)
Monash University (Parkville Campus)
4-Aminopiperidine ureas as potent selective agonists of the human beta(3)-adrenergic receptor.
Bioorg Med Chem Lett 11: 3123-7 (2001)
Wyeth-Ayerst Research
Synthesis and biological activity of L-tyrosine-based PPARgamma agonists with reduced molecular weight.
Bioorg Med Chem Lett 11: 3111-3 (2001)
Glaxosmithkline
Design, synthesis, and SAR of heterocycle-containing antagonists of the human CCR5 receptor for the treatment of HIV-1 infection.
Bioorg Med Chem Lett 11: 3103-6 (2001)
Merck Research Laboratories
Discovery of human CCR5 antagonists containing hydantoins for the treatment of HIV-1 infection.
Bioorg Med Chem Lett 11: 3099-102 (2001)
Merck Research Laboratories
A new dimeric stilbene with tyrosinase inhibitiory activity from Artocarpus gomezianus.
J Nat Prod 64: 1457-9 (2001)
Chulalongkorn University
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
Biochem Biophys Res Commun 289: 580-5 (2001)
Schering-Plough Research Institute
Functional calcitonin gene-related peptide subtype 2 receptors in porcine coronary arteries are identified as calcitonin gene-related peptide subtype 1 receptors by radioligand binding and reverse transcription-polymerase chain reaction.
J Pharmacol Exp Ther 299: 1086-94 (2001)
Creighton University
N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-nitrophenyl) cyclohexanecarboxamide: a novel pre- and postsynaptic 5-hydroxytryptamine(1A) receptor antagonist active on the lower urinary tract.
J Pharmacol Exp Ther 299: 1027-37 (2001)
Recordati
Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists.
J Pharmacol Exp Ther 299: 908-14 (2001)
Vrije Universiteit
The pharmacological profile of (R)-3,4-dihydro-N-isopropyl-3-(N-isopropyl-N-propylamino)-2H-1-benzopyran-5-carboxamide, a selective 5-hydroxytryptamine(1A) receptor agonist.
J Pharmacol Exp Ther 299: 883-93 (2001)
Astrazeneca R&D
Identification of a novel family of nucleosides that specifically inhibit HIV-1 reverse transcriptase.
Bioorg Med Chem Lett 11: 3085-8 (2001)
Instituto De QuíMica MéDica (Csic)
Dual neurokinin NK(1)/NK(2) antagonists: N-[(R,R)-(E)-1-arylmethyl-3-(2-oxo-azepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamides and 3-[N'-3,5-bis(trifluoromethyl)benzoyl-N-arylmethyl-N'-methylhydrazino]-N-[(R)-2-oxo-azepan-3-yl]propionamides.
Bioorg Med Chem Lett 11: 3081-4 (2001)
Novartis Pharma
Synthesis and binding affinities of 2 beta-(3-iodoallyloxycarbonyl)-3 beta-(4-substituted-aryl)tropane analogues as ligands for the dopamine transporter studies.
Bioorg Med Chem Lett 11: 3077-80 (2001)
Inha University
A novel class of highly potent, selective, and non-peptidic inhibitor of Ras farnesyltransferase (FTase).
Bioorg Med Chem Lett 11: 3069-72 (2001)
Lgci
Synthesis and biological evaluation of a series of novel N- or O-fluoroalkyl derivatives of tropane: potential positron emission tomography (PET) imaging agents for the dopamine transporter.
Bioorg Med Chem Lett 11: 3049-53 (2001)
Alcohol And Drug Abuse Research Center
BMS-196085: a potent and selective full agonist of the human beta(3) adrenergic receptor.
Bioorg Med Chem Lett 11: 3041-4 (2001)
Bristol-Myers Squibb Pharmaceutical Research Institute
Beta 3 agonists. Part 1: evolution from inception to BMS-194449.
Bioorg Med Chem Lett 11: 3035-9 (2001)
Bristol-Myers Squibb Pharmaceutical Research Institute
2-Aryl indole NK(1) antagonists: optimisation of the amide substituent.
Bioorg Med Chem Lett 11: 3031-4 (2001)
Merck Sharp & Dohme Research Laboratories
Synthesis of antitumor dendritic imides.
Bioorg Med Chem Lett 11: 3027-9 (2001)
University San Pablo-Ceu
7-Nitrobenzofurazan (NBD) derivatives of 5'-N-ethylcarboxamidoadenosine (NECA) as new fluorescent probes for human A(3) adenosine receptors.
Bioorg Med Chem Lett 11: 3023-6 (2001)
Universit£
Discovery and evaluation of piperidinyl carboxylic acid derivatives as potent alpha(4)beta(1) integrin antagonists.
Bioorg Med Chem Lett 11: 3019-21 (2001)
Bayer
Cyclopenta[g]quinazoline-based antifolates: the effect of the chirality at the 6-position on the inhibition of thymidylate synthase (TS).
Bioorg Med Chem Lett 11: 3015-7 (2001)
The Institute Of Cancer Research
Determination and use of a transition state for the enzyme estrone sulfatase (ES) from a proposed reaction mechanism.
Bioorg Med Chem Lett 11: 3001-5 (2001)
Kingston University
Discovery of a N'-hydroxyphenylformamidine derivative HET0016 as a potent and selective 20-HETE synthase inhibitor.
Bioorg Med Chem Lett 11: 2993-5 (2001)
Taisho Pharmaceutical
Synthesis and quantitative structure-activity relationships of fluorine-containing 4,4-dihydroxylmethyl-2-aryliminooxazo(thiazo)lidines as trehalase inhibitors.
J Agric Food Chem 49: 5279-84 (2001)
Dalian University Of Technology
An orally active, water-soluble neurokinin-1 receptor antagonist suitable for both intravenous and oral clinical administration.
J Med Chem 44: 4296-9 (2001)
Merck
5,6-Diphenylpyridazine derivatives as acyl-CoA:cholesterol acyltransferase inhibitors.
J Med Chem 44: 4292-5 (2001)
Università
Role of hydrophilic interaction in binding of hydroxylated 3-deoxy C(19) steroids to the active site of aromatase.
J Med Chem 44: 4277-83 (2001)
Tohoku Pharmaceutical University
A prodrug form of a Plasmodium falciparum glutathione reductase inhibitor conjugated with a 4-anilinoquinoline.
J Med Chem 44: 4268-76 (2001)
Umr 8525 Cnrs-Université
Design of selective and soluble inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
J Med Chem 44: 4252-67 (2001)
Glaxosmithkline
Estrogen receptor-beta potency-selective ligands: structure-activity relationship studies of diarylpropionitriles and their acetylene and polar analogues.
J Med Chem 44: 4230-51 (2001)
University Of Illinois
5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1) receptor antagonists: structure-activity relationship studies on the central 1,3-dioxoperhydropyrido[1,2-c]pyrimidine scaffold.
J Med Chem 44: 4196-206 (2001)
Instituto De Qu£Mica M£Dica (Csic)
Design and pharmacological activity of phosphinic acid based NAALADase inhibitors.
J Med Chem 44: 4170-5 (2001)
Guilford Pharmaceuticals
Synthesis and biological evaluation of prostaglandin-F alkylphosphinic acid derivatives as bone anabolic agents for the treatment of osteoporosis.
J Med Chem 44: 4157-69 (2001)
Procter & Gamble Pharmaceuticals
Neoceptor concept based on molecular complementarity in GPCRs: a mutant adenosine A(3) receptor with selectively enhanced affinity for amine-modified nucleosides.
J Med Chem 44: 4125-36 (2001)
National Institute Of Diabetes And Digestive And Kidney Diseases
Novel agouti-related-protein-based melanocortin-1 receptor antagonist.
J Med Chem 44: 4114-24 (2001)
University Of Florida
The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors.
J Med Chem 44: 4092-113 (2001)
Purdue University
Methyl analogues of the experimental Alzheimer drug phenserine: synthesis and structure/activity relationships for acetyl- and butyrylcholinesterase inhibitory action.
J Med Chem 44: 4062-71 (2001)
National Institutes Of Health
Monosaccharide-linked inhibitors of O(6)-methylguanine-DNA methyltransferase (MGMT): synthesis, molecular modeling, and structure-activity relationships.
J Med Chem 44: 4050-61 (2001)
German Cancer Research Center
Discovery and biological evaluation of a new family of potent inhibitors of the dual specificity protein phosphatase Cdc25.
J Med Chem 44: 4042-9 (2001)
University Of Pittsburgh
Design, synthesis, and biological activity of methoctramine-related polyamines as putative G(i) protein activators.
J Med Chem 44: 4035-8 (2001)
University Of Bologna
N-[3-(2-Dimethylaminoethyl)-2-methyl-1H- indol-5-yl]-4-fluorobenzamide: a potent, selective, and orally active 5-HT(1F) receptor agonist potentially useful for migraine therapy.
J Med Chem 44: 4031-4 (2001)
Eli Lilly
Di-, tri- and tetra-5'-O-phosphorothioadenosyl substituted polyols as inhibitors of Fhit: Importance of the alpha-beta bridging oxygen and beta phosphorus replacement.
BMC Chem Biol 1: 3 (2001)
Kimmel Cancer Center
Glycosylasparaginase inhibition studies: competitive inhibitors, transition state mimics, noncompetitive inhibitors.
J Enzym Inhib 16: 269-74 (2001)
University Of North Carolina
Structure-activity studies on nociceptin analogues: ORL1 receptor binding and biological activity of cyclic disulfide-containing analogues of nociceptin peptides.
J Med Chem 44: 4015-8 (2001)
Tohoku Pharmaceutical University
Synthesis and screening for antiacetylcholinesterase activity of (1-benzyl-4-oxopiperidin-3-ylidene)methylindoles and -pyrroles related to donepezil.
J Med Chem 44: 4011-4 (2001)
Università
Discovery of a series of nonpeptide small molecules that inhibit the binding of insulin-like growth factor (IGF) to IGF-binding proteins.
J Med Chem 44: 4001-10 (2001)
Neurocrine Biosciences
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 5. Highly selective, potent, and orally active ET(A) antagonists.
J Med Chem 44: 3978-84 (2001)
Abbott Laboratories
Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity.
J Med Chem 44: 3965-77 (2001)
Wyeth-Ayerst Research
Structure-activity studies of the Phe(4) residue of nociceptin(1-13)-NH(2): identification of highly potent agonists of the nociceptin/orphanin FQ receptor.
J Med Chem 44: 3956-64 (2001)
University Of Ferrara
Structure-affinity relationships of a unique nicotinic ligand: N(1)-dimethyl-N(4)-phenylpiperazinium iodide (DMPP).
J Med Chem 44: 3946-55 (2001)
Universit£
Synthesis and biological evaluation of tropane-like 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909) analogues.
J Med Chem 44: 3937-45 (2001)
National Institute Of Diabetes And Digestive And Kidney Diseases
Antitumor Agents. 211. Fluorinated 2-phenyl-4-quinolone derivatives as antimitotic antitumor agents.
J Med Chem 44: 3932-6 (2001)
University Of North Carolina
Pseudoproline-containing analogues of morphiceptin and endomorphin-2: evidence for a cis Tyr-Pro amide bond in the bioactive conformation.
J Med Chem 44: 3896-903 (2001)
University Of Lausanne
N-Arylsulfonylindole derivatives as serotonin 5-HT(6) receptor ligands.
J Med Chem 44: 3881-95 (2001)
Merck Sharp & Dohme Research Laboratories
Iridals are a novel class of ligands for phorbol ester receptors with modest selectivity for the RasGRP receptor subfamily.
J Med Chem 44: 3872-80 (2001)
University Of Michigan Cancer Center
Exploiting subsite S1 of trypsin-like serine proteases for selectivity: potent and selective inhibitors of urokinase-type plasminogen activator.
J Med Chem 44: 3856-71 (2001)
Axys Pharmaceuticals
Three-dimensional quantitative structure-activity relationship (3D-QSAR) models for a novel class of piperazine-based stromelysin-1 (MMP-3) inhibitors: applying a"divide and conquer" strategy.
J Med Chem 44: 3849-55 (2001)
University Of Missouri St. Louis
Synthesis and activity of novel and selective I(Ks)-channel blockers.
J Med Chem 44: 3831-7 (2001)
Aventis Pharma Deutschland
Acetylcholinesterase inhibitors: SAR and kinetic studies on omega-[N-methyl-N-(3-alkylcarbamoyloxyphenyl)methyl]aminoalkoxyaryl derivatives.
J Med Chem 44: 3810-20 (2001)
University Of Bologna
Modeling of poly(ADP-ribose)polymerase (PARP) inhibitors. Docking of ligands and quantitative structure-activity relationship analysis.
J Med Chem 44: 3786-94 (2001)
Università
Design and synthesis of 4-substituted benzamides as potent, selective, and orally bioavailable I(Ks) blockers.
J Med Chem 44: 3764-7 (2001)
TBA
Novel lead generation through hypothetical pharmacophore three-dimensional database searching: discovery of isoflavonoids as nonsteroidal inhibitors of rat 5 alpha-reductase.
J Med Chem 44: 3759-63 (2001)
TBA
Functional characterization of human organic anion transporting polypeptide B (OATP-B) in comparison with liver-specific OATP-C.
Pharm Res 18: 1262-9 (2001)
Kanazawa University
Makaluvamine P, a new cytotoxic pyrroloiminoquinone from Zyzzya cf. fuliginosa.
J Nat Prod 64: 1354-6 (2001)
Universit£
Antimalarial (+)-trans-hexahydrodibenzopyran derivatives from Machaerium multiflorum.
J Nat Prod 64: 1322-5 (2001)
University Of Mississippi
Inhibition of leukocyte functions by the alkaloid isaindigotone from Isatis indigotica and some new synthetic derivatives.
J Nat Prod 64: 1297-300 (2001)
Universidad De Murcia
Catalytic inhibition of topoisomerase IIalpha by demethylzeylasterone, a 6-oxophenolic triterpenoid from Kokoona zeylanica.
J Nat Prod 64: 1294-6 (2001)
University Of Arizona
Aromatase inhibitors from Broussonetia papyrifera.
J Nat Prod 64: 1286-93 (2001)
University Of Illinois At Chicago
Fipronil-based photoaffinity probe for Drosophila and human beta 3 GABA receptors.
Bioorg Med Chem Lett 11: 2979-81 (2001)
University Of California
The discovery of anthranilic acid-based MMP inhibitors. Part 3: incorporation of basic amines.
Bioorg Med Chem Lett 11: 2975-8 (2001)
Wyeth-Ayerst Research
3-Aryl-4-aryloyl-1-(1H-imidazol-5-yl)methylpyrrole, a novel class of farnesyltransferase inhibitors.
Bioorg Med Chem Lett 11: 2963-5 (2001)
Lgci
Identification of a series of PPAR gamma/delta dual agonists via solid-phase parallel synthesis.
Bioorg Med Chem Lett 11: 2959-62 (2001)
Glaxosmithkline
Design and synthesis of potent and selective inhibitors of integrin VLA-4.
Bioorg Med Chem Lett 11: 2955-8 (2001)
Novartis Institute For Biomedical Research
Discovery and parallel synthesis of a new class of cathepsin K inhibitors.
Bioorg Med Chem Lett 11: 2951-4 (2001)
Bayer Research Center
Design, synthesis, and SAR of amino acid derivatives as factor Xa inhibitors.
Bioorg Med Chem Lett 11: 2947-50 (2001)
Cor Therapeutics
Cantharimides: a new class of modified cantharidin analogues inhibiting protein phosphatases 1 and 2A.
Bioorg Med Chem Lett 11: 2941-6 (2001)
The University Of Newcastle
Discovery of selective hydroxamic acid inhibitors of tumor necrosis factor-alpha converting enzyme.
Bioorg Med Chem Lett 11: 2907-10 (2001)
Abbott Laboratories
A unique ring-expanded acyclic nucleoside analogue that inhibits both adenosine deaminase (ADA) and guanine deaminase (GDA; guanase): synthesis and enzyme inhibition studies of 4,6-diamino-8H-1-hydroxyethoxymethyl-8-iminoimidazo[4,5-e][1,3]diazepine.
Bioorg Med Chem Lett 11: 2893-6 (2001)
University Of Maryland
Characterization of ochratoxin A transport by human organic anion transporters.
Life Sci 69: 2123-35 (2001)
Kyorin University
Mercapturic acids (N-acetylcysteine S-conjugates) as endogenous substrates for the renal organic anion transporter-1.
Mol Pharmacol 60: 1091-9 (2001)
University Of Rochester School Of Medicine And Dentistry
The farnesyl protein transferase inhibitor SCH66336 is a potent inhibitor of MDR1 product P-glycoprotein.
Cancer Res 61: 7525-9 (2001)
Schering-Plough Research Institute
Synthesis of 1-benzyl-3-(5'-hydroxymethyl-2'-furyl)indazole analogues as novel antiplatelet agents.
J Med Chem 44: 3746-9 (2001)
Institute Of Pharmaceutical Chemistry
Hydrazinonaphthalene and azonaphthalene thrombopoietin mimics are nonpeptidyl promoters of megakaryocytopoiesis.
J Med Chem 44: 3730-45 (2001)
Glaxosmithkline
Design, synthesis, and biological evaluation of novel nucleoside and nucleotide analogues as agents against DNA viruses and/or retroviruses.
J Med Chem 44: 3710-20 (2001)
Academia Sinica
Selective, high affinity peptide antagonists of alpha-melanotropin action at human melanocortin receptor 4: their synthesis and biological evaluation in vitro.
J Med Chem 44: 3665-72 (2001)
Merck Research Laboratories
Design, synthesis, and evaluation of a long-acting, potent analogue of gonadotropin-releasing hormone.
J Med Chem 44: 3645-52 (2001)
Institute Of Science
Synthesis of sulfaphenazole derivatives and their use as inhibitors and tools for comparing the active sites of human liver cytochromes P450 of the 2C subfamily.
J Med Chem 44: 3622-31 (2001)
Université
Alpha-amino acid phenolic ester derivatives: novel water-soluble general anesthetic agents which allosterically modulate GABA(A) receptors.
J Med Chem 44: 3582-91 (2001)
Organon Research And Development Group
Toward the quantitative prediction of T-cell epitopes: coMFA and coMSIA studies of peptides with affinity for the class I MHC molecule HLA-A*0201.
J Med Chem 44: 3572-81 (2001)
Edward Jenner Institute For Vaccine Research
Interaction of 2,3-dimercapto-1-propane sulfonate with the human organic anion transporter hOAT1.
J Pharmacol Exp Ther 299: 741-7 (2001)
University Of Arizona
OPC-28326, a selective femoral vasodilator, is an alpha2C-adrenoceptor-selective antagonist.
J Pharmacol Exp Ther 299: 652-8 (2001)
Otsuka Maryland Research Institute
Derivatives of 17-(2-methylallyl)-substituted noroxymorphone: variation of the delta address and its effects on affinity and selectivity for the delta opioid receptor.
Bioorg Med Chem Lett 11: 2883-5 (2001)
Niddk
Design and synthesis of Pfmrk inhibitors as potential antimalarial agents.
Bioorg Med Chem Lett 11: 2875-8 (2001)
The Ohio State University
2-(Anilinomethyl)imidazolines as alpha(1)-adrenoceptor agonists: the identification of alpha(1A) subtype selective 2'-carboxylic acid esters and amides.
Bioorg Med Chem Lett 11: 2871-4 (2001)
Glaxosmithkline
Pyrimidinylimidazole inhibitors of p38: cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity.
Bioorg Med Chem Lett 11: 2867-70 (2001)
Glaxosmithkline
Dopaminergic 7-aminotetrahydroindolizines: ex-chiral pool synthesis and preferential D3 receptor binding.
Bioorg Med Chem Lett 11: 2863-6 (2001)
Friedrich-Alexander University
Synthesis and In vitro binding affinities of 1-azabicyclic compounds as muscarinic ligands.
Bioorg Med Chem Lett 11: 2855-7 (2001)
Seoul National University
Potent, low molecular weight thrombin receptor antagonists.
Bioorg Med Chem Lett 11: 2851-3 (2001)
Schering-Plough Research Institute
Design and synthesis of a novel class of histone deacetylase inhibitors.
Bioorg Med Chem Lett 11: 2847-50 (2001)
Methylgene
Novel (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides with high affinity and selectivity for the 5-HT(6) receptor.
Bioorg Med Chem Lett 11: 2843-6 (2001)
Glaxosmithkline
Synthesis, crystal structure determination, and biological properties of the DNA-dependent protein kinase (DNA-PK) inhibitor 3-cyano-6-hydrazonomethyl-5-(4-pyridyl)pyrid-[1H]-2-one (OK-1035).
Bioorg Med Chem Lett 11: 2837-41 (2001)
Newcastle University
A designed antagonist of the thyroid hormone receptor.
Bioorg Med Chem Lett 11: 2821-5 (2001)
University Of California
Design, synthesis, and biological activity of diiminoisoindolines as complement component 3a antagonists.
Bioorg Med Chem Lett 11: 2817-20 (2001)
The R. W. Johnson Pharmaceutical Research Institute
3-D-QSAR/CoMFA and recognition models of benzimidazole derivatives at the 5-HT(4) receptor.
Bioorg Med Chem Lett 11: 2807-11 (2001)
Universidad Complutense
Antiviral drug design: computational analyses of the effects of the L100I mutation for HIV-RT on the binding of NNRTIs.
Bioorg Med Chem Lett 11: 2799-802 (2001)
Yale University
Structure-based design of caspase-1 inhibitor containing a diphenyl ether sulfonamide.
Bioorg Med Chem Lett 11: 2779-82 (2001)
Pfizer
Discovery of heterocyclic ureas as a new class of raf kinase inhibitors: identification of a second generation lead by a combinatorial chemistry approach.
Bioorg Med Chem Lett 11: 2775-8 (2001)
Bayer Research Center
Discovery of novel, orally active dual NK1/NK2 antagonists.
Bioorg Med Chem Lett 11: 2769-73 (2001)
Astrazeneca Pharmaceuticals
Simplified catechin-gallate inhibitors of HIV-1 reverse transcriptase.
Bioorg Med Chem Lett 11: 2763-7 (2001)
University Of Toledo
Synthesis and progesterone receptor antagonist activities of 6-aryl benzimidazolones and benzothiazolones.
Bioorg Med Chem Lett 11: 2747-50 (2001)
Wyeth-Ayerst Research
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 2: lead optimization affording selective, orally bioavailable compounds with potent anti-HIV activity.
Bioorg Med Chem Lett 11: 2741-5 (2001)
Merck Research Laboratories
Mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine abuse: synthesis and opioid receptor binding affinity of N-substituted derivatives of morphinan.
Bioorg Med Chem Lett 11: 2735-40 (2001)
Harvard Medical School
Small molecule somatostatin receptor subtype-2 antagonists.
Bioorg Med Chem Lett 11: 2731-4 (2001)
Pfizer
Small molecule/nucleic acid affinity chromatography: application for the identification of telomerase inhibitors which target its key RNA/DNA heteroduplex.
Bioorg Med Chem Lett 11: 2727-30 (2001)
University Of Missouri
alpha-Alkyl-alpha-amino-beta-sulphone hydroxamates as potent MMP inhibitors that spare MMP-1.
Bioorg Med Chem Lett 11: 2723-5 (2001)
Pfizer
alpha-Amino-beta-sulphone hydroxamates as potent MMP-13 inhibitors that spare MMP-1.
Bioorg Med Chem Lett 11: 2719-22 (2001)
Pfizer
Synthesis of N-propargylphenelzine and analogues as neuroprotective agents.
Bioorg Med Chem Lett 11: 2715-7 (2001)
Cv Technologies
The discovery of sulfonylated dipeptides as potent VLA-4 antagonists.
Bioorg Med Chem Lett 11: 2709-13 (2001)
Merck Research Laboratories
Discovery and initial structure-activity relationships of trisubstituted ureas as thrombin receptor (PAR-1) antagonists.
Bioorg Med Chem Lett 11: 2691-6 (2001)
Merck Research Laboratories
Naphthalene derivatives: A new series of selective cyclooxygenase-2 inhibitors.
Bioorg Med Chem Lett 11: 2687-90 (2001)
RhôNe-Poulenc Rorer
Predicting and harnessing protein flexibility in the design of species-specific inhibitors of thymidylate synthase.
Chem Biol 8: 981-95 (2001)
University Of California San Francisco
Long lasting antinociceptive properties of enkephalin degrading enzyme (NEP and APN) inhibitor prodrugs.
J Med Chem 44: 3523-30 (2001)
University Of Paris
1,2-Benzothiazine 1,1-dioxide P(2)-P(3) peptide mimetic aldehyde calpain I inhibitors.
J Med Chem 44: 3488-503 (2001)
Cephalon
Selective inhibition of ICAM-1 and E-selectin expression in human endothelial cells. 2. Aryl modifications of 4-(aryloxy)thieno[2,3-c]pyridines with fine-tuning at C-2 carbamides.
J Med Chem 44: 3469-87 (2001)
Abbott Laboratories
Synthesis and biological evaluation of s-triazine substituted polyamines as potential new anti-trypanosomal drugs.
J Med Chem 44: 3440-52 (2001)
Cardiff University
Statistical molecular design, parallel synthesis, and biological evaluation of a library of thrombin inhibitors.
J Med Chem 44: 3424-39 (2001)
Astrazeneca
Are free energy calculations useful in practice? A comparison with rapid scoring functions for the p38 MAP kinase protein system.
J Med Chem 44: 3417-23 (2001)
Vertex Pharmaceuticals
Synthesis of novel, potent, diol-based HIV-1 protease inhibitors via intermolecular pinacol homocoupling of (2S)-2-benzyloxymethyl-4-phenylbutanal.
J Med Chem 44: 3407-16 (2001)
Stockholm University
Synthesis of potent C(2)-symmetric, diol-based hiv-1 protease inhibitors. Investigation of thioalkyl and thioaryl P1/P1' substituents.
J Med Chem 44: 3402-6 (2001)
Stockholm University
From hit to lead. Analyzing structure-profile relationships.
J Med Chem 44: 3391-401 (2001)
Universities Of Lille
From hit to lead. Combining two complementary methods for focused library design. Application to mu opiate ligands.
J Med Chem 44: 3378-90 (2001)
Universities Of Lille
Potent and selective ET-A antagonists. 2. Discovery and evaluation of potent and water soluble N-(6-(2-(aryloxy)ethoxy)-4-pyrimidinyl)sulfonamide derivatives.
J Med Chem 44: 3369-77 (2001)
Tanabe Seiyaku
Potent and selective ET-A antagonists. 1. Syntheses and structure-activity relationships of N-(6-(2-(aryloxy)ethoxy)-4-pyrimidinyl)sulfonamide derivatives.
J Med Chem 44: 3355-68 (2001)
Tanabe Seiyaku
Discovery of macrocyclic hydroxamic acids containing biphenylmethyl derivatives at P1', a series of selective TNF-alpha converting enzyme inhibitors with potent cellular activity in the inhibition of TNF-alpha release.
J Med Chem 44: 3351-4 (2001)
Dupont Pharmaceuticals
Design and synthesis of a series of (2R)-N(4)-hydroxy-2-(3-hydroxybenzyl)-N(1)- [(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide derivatives as potent, selective, and orally bioavailable aggrecanase inhibitors.
J Med Chem 44: 3347-50 (2001)
Dupont Pharmaceuticals
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. II. Discovery of 1-[(2,4-dimethyl-3-pyridinyl)carbonyl]-4- methyl-4-[3(S)-methyl-4-[1(S)-[4-(trifluoromethyl)phenyl]ethyl]-1-piperazinyl]- piperidine N1-oxide (Sch-350634), an orally bioavailable, potent CCR5 antagonist.
J Med Chem 44: 3343-6 (2001)
Schering-Plough Research Institute
Discovery of 4-[(Z)-(4-bromophenyl)- (ethoxyimino)methyl]-1'-[(2,4-dimethyl-3- pyridinyl)carbonyl]-4'-methyl-1,4'- bipiperidine N-oxide (SCH 351125): an orally bioavailable human CCR5 antagonist for the treatment of HIV infection.
J Med Chem 44: 3339-42 (2001)
Schering-Plough Research Institute
Resolution, configurational assignment, and enantiopharmacology at glutamate receptors of 2-amino-3-(3-carboxy-5-methyl-4-isoxazolyl)propionic acid (ACPA) and demethyl-ACPA.
Chirality 13: 523-32 (2001)
The Royal Danish School Of Pharmacy
Fluoroaromatic-fluoroaromatic interactions between inhibitors bound in the crystal lattice of human carbonic anhydrase II.
J Am Chem Soc 123: 9620-7 (2001)
University Of Pennsylvania
Crystal structure of Staphylococcus aureus tyrosyl-tRNA synthetase in complex with a class of potent and specific inhibitors.
Protein Sci 10: 2008-16 (2001)
Gsk
Synthesis of potential antidipsotropic isoflavones: inhibitors of the mitochondrial monoamine oxidase-aldehyde dehydrogenase pathway.
J Med Chem 44: 3320-8 (2001)
Harvard Medical School
Arylcyclopropanecarboxyl guanidines as novel, potent, and selective inhibitors of the sodium hydrogen exchanger isoform-1.
J Med Chem 44: 3302-10 (2001)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and biological evaluation of sialylmimetics as rotavirus inhibitors.
J Med Chem 44: 3292-301 (2001)
Griffith University (Gold Coast Campus)
1-[2-methoxy-5-(3-phenylpropyl)]-2-aminopropane unexpectedly shows 5-HT(2A) serotonin receptor affinity and antagonist character.
J Med Chem 44: 3283-91 (2001)
Virginia Commonwealth University
Structure-based design and synthesis of potent matrix metalloproteinase inhibitors derived from a 6H-1,3,4-thiadiazine scaffold.
J Med Chem 44: 3231-43 (2001)
UniversitäT Bielefeld
Three-dimensional quantitative structure-activity relationships of cyclo-oxygenase-2 (COX-2) inhibitors: a comparative molecular field analysis.
J Med Chem 44: 3223-30 (2001)
Universit£
Synthesis of a tetronic acid library focused on inhibitors of tyrosine and dual-specificity protein phosphatases and its evaluation regarding VHR and cdc25B inhibition.
J Med Chem 44: 3216-22 (2001)
Tohoku University
A structure-based design approach to the development of novel, reversible AChE inhibitors.
J Med Chem 44: 3203-15 (2001)
Syngenta
Multispecific substrate recognition of kidney-specific organic anion transporters OAT-K1 and OAT-K2.
J Pharmacol Exp Ther 299: 261-7 (2001)
Kyoto University Hospital
Troglitazone-induced intrahepatic cholestasis by an interference with the hepatobiliary export of bile acids in male and female rats. Correlation with the gender difference in troglitazone sulfate formation and the inhibition of the canalicular bile salt export pump (Bsep) by troglitazone and trogl
Toxicology 167: 83-98 (2001)
F. Hoffmann-La Roche
Antiprotozoal and cytotoxicity evaluation of sulfonamide and urea analogues of quinacrine.
Bioorg Med Chem Lett 11: 2655-7 (2001)
University Of Cape Town
Selective heterocyclic amidine inhibitors of human inducible nitric oxide synthase.
Bioorg Med Chem Lett 11: 2651-3 (2001)
Pharmacia
Synthesis of a reported calpain inhibitor isolated from Streptomyces griseus.
Bioorg Med Chem Lett 11: 2647-9 (2001)
The University Of Tennessee Health Science Center
New inhibitors of the thioredoxin-thioredoxin reductase system based on a naphthoquinone spiroketal natural product lead.
Bioorg Med Chem Lett 11: 2637-41 (2001)
University Of Pittsburgh
Synthesis and acetylcholinesterase inhibition of 5-desamino huperzine A derivatives.
Bioorg Med Chem Lett 11: 2627-30 (2001)
Universit£T Wien
1,2,4-triazolo[3,4-a]pyridine as a novel, constrained template for fibrinogen receptor (GPIIb/IIIa) antagonists.
Bioorg Med Chem Lett 11: 2619-22 (2001)
The R. W. Johnson Pharmaceutical Research Institute
Potent peptide alpha-ketohydroxamate inhibitors of recombinant human calpain I.
Bioorg Med Chem Lett 11: 2615-7 (2001)
Cephalon
Orally bioavailable, indole-based nonpeptide GnRH receptor antagonists with high potency and functional activity.
Bioorg Med Chem Lett 11: 2597-602 (2001)
Merck Research Laboratories
Isoxazolyl, oxazolyl, and thiazolylpropionic acid derivatives as potent alpha(4)beta(1) integrin antagonists.
Bioorg Med Chem Lett 11: 2593-6 (2001)
Pfizer
Synthesis and in vitro evaluation of a series of diketopiperazine inhibitors of plasminogen activator inhibitor-1.
Bioorg Med Chem Lett 11: 2589-92 (2001)
Xenova
Asymmetric synthesis of BB-3497--a potent peptide deformylase inhibitor.
Bioorg Med Chem Lett 11: 2585-8 (2001)
British Biotech Pharmaceuticals
Solid-Phase synthesis of a library constructed of aromatic phosphate, long alkyl chains and tryptophane components, and identification of potent dipeptide telomerase inhibitors.
Bioorg Med Chem Lett 11: 2581-4 (2001)
Kyushu University
Novel 3-dodecanoylindole-2-carboxylic acid inhibitors of cytosolic phospholipase A(2).
Bioorg Med Chem Lett 11: 2569-72 (2001)
University Of MüNster
Combinatorial synthesis of SSAO inhibitors using sonogashira coupling: SAR of aryl propargylic amines.
Bioorg Med Chem Lett 11: 2565-8 (2001)
University Of Technology
Glutamyl-gamma-boronate inhibitors of bacterial Glu-tRNA(Gln) amidotransferase.
Bioorg Med Chem Lett 11: 2561-4 (2001)
Dupont Pharmaceuticals
New leads for selective inhibitors of alpha-L-fucosidases. Synthesis and glycosidase inhibitory activities of [(2R,3S,4R)-3,4-dihydroxypyrrolidin-2-yl]furan derivatives.
Bioorg Med Chem Lett 11: 2555-9 (2001)
Universidad De Sevilla
Substituted imidazoles as glucagon receptor antagonists.
Bioorg Med Chem Lett 11: 2549-53 (2001)
Merck Research Laboratories
Benzamide bioisosteres incorporating dihydroheteroazole substructures: EPC synthesis and SAR leading to a selective dopamine D4 receptor partial agonist (FAUC 179).
Bioorg Med Chem Lett 11: 2533-6 (2001)
Friedrich-Alexander University
Synthesis and biological data of 4-amino-1-(2-chloro-2-phenylethyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid ethyl esters, a new series of A1-adenosine receptor (A1AR) ligands.
Bioorg Med Chem Lett 11: 2529-31 (2001)
Facoltà
Hydrophobicity, a physicochemical factor in the inhibition of the enzyme estrone sulfatase (ES).
Bioorg Med Chem Lett 11: 2525-8 (2001)
Kingston University
Furans with basic side chains: synthesis and biological evaluation of a novel series of antagonists with selectivity for the estrogen receptor alpha.
Bioorg Med Chem Lett 11: 2521-4 (2001)
University Of Illinois
Synthesis and evaluation of the sunflower derived trypsin inhibitor as a potent inhibitor of the type II transmembrane serine protease, matriptase.
Bioorg Med Chem Lett 11: 2515-9 (2001)
National Cancer Institute-Frederick
Inhibitors of bacterial tyrosyl tRNA synthetase: synthesis of carbocyclic analogues of the natural product SB-219383.
Bioorg Med Chem Lett 11: 2499-502 (2001)
Glaxosmithkline
Derivatives of (2R,3R,4S)-2-aminomethylpyrrolidine-3,4-diol are selective alpha-mannosidase inhibitors.
Bioorg Med Chem Lett 11: 2489-93 (2001)
Section De Chimie De L'Universit£
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4: synthesis and structure-activity relationships for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl)-N-(benzyloxycarbonyl)amino)piperidin-1-yl)butanes.
Bioorg Med Chem Lett 11: 2475-9 (2001)
Merck Research Laboratories
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 3: a proposed pharmacophore model for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-[4-(substituted)piperidin-1-yl]butanes.
Bioorg Med Chem Lett 11: 2469-73 (2001)
Merck Research Laboratories
Design and synthesis of new inhibitors of HIV-1 protease dimerization with conformationally constrained templates.
Bioorg Med Chem Lett 11: 2465-8 (2001)
Kyoto Pharmaceutical University
The discovery of novel, potent and selective PDE5 inhibitors.
Bioorg Med Chem Lett 11: 2461-4 (2001)
Bristol-Myers Squibb Pharmaceutical Research Institute
Alpha-ketoester-based photobiological switches: synthesis, peptide chain extension and assay against alpha-chymotrypsin.
Bioorg Med Chem Lett 11: 2441-4 (2001)
University Of Canterbury
Synthesis and biological evaluation of clitocine analogues as adenosine kinase inhibitors.
Bioorg Med Chem Lett 11: 2419-22 (2001)
Abbott Laboratories
The molecular and behavioral pharmacology of the orphanin FQ/nociceptin peptide and receptor family.
Pharmacol Rev 53: 381-415 (2001)
Mcgill University
Coumarins derivatives as dual inhibitors of acetylcholinesterase and monoamine oxidase.
J Med Chem 44: 3195-8 (2001)
Universit£
Design and synthesis of [(2,3-dichlorophenyl)piperazin-1-yl]alkylfluorenylcarboxamides as novel ligands selective for the dopamine D3 receptor subtype.
J Med Chem 44: 3175-86 (2001)
National Institute On Drug Abuse-Intramural Research Program
Identification of alkylidene hydrazides as glucagon receptor antagonists.
J Med Chem 44: 3141-9 (2001)
Pfizer
Exploration of novel aryl binding sites of farnesyltransferase using molecular modeling and benzophenone-based farnesyltransferase inhibitors.
J Med Chem 44: 3117-24 (2001)
Philipps-UniversitäT Marburg
A new approach to search for the bioactive conformation of glucagon: positional cyclization scanning.
J Med Chem 44: 3109-16 (2001)
University Of Arizona
Acyclic and cyclopropyl analogues of adenosine bisphosphate antagonists of the P2Y1 receptor: structure-activity relationships and receptor docking.
J Med Chem 44: 3092-108 (2001)
National Institute Of Diabetes
Design and synthesis of potent C(2)-symmetric diol-based HIV-1 protease inhibitors: effects of fluoro substitution.
J Med Chem 44: 3083-91 (2001)
Linkoping University
Design and synthesis of matrix metalloproteinase inhibitors guided by molecular modeling. Picking the S(1) pocket using conformationally constrained inhibitors.
J Med Chem 44: 3074-82 (2001)
Université
N-Aryl sulfonyl homocysteine hydroxamate inhibitors of matrix metalloproteinases: further probing of the S(1), S(1)', and S(2)' pockets.
J Med Chem 44: 3066-73 (2001)
Université
Determination of the binding specificity of an integral membrane protein by saturation transfer difference NMR: RGD peptide ligands binding to integrin alphaIIbbeta3.
J Med Chem 44: 3059-65 (2001)
University Of Hamburg
[2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists.
J Med Chem 44: 3048-53 (2001)
Clinical Research Institute Of Montreal
Identification of a series of oxadiazole-substituted alpha-isopropoxy phenylpropanoic acids with activity on PPARalpha, PPARgamma, and PPARdelta.
Bioorg Med Chem Lett 11: 2385-8 (2001)
Glaxosmithkline
Drug design, synthesis, and evaluation of a non-sugar-based selectin antagonist.
Bioorg Med Chem Lett 11: 2365-7 (2001)
Organon K.K.
A novel class of inhibitors for steroid 5alpha-reductase: synthesis and evaluation of umbelliferone derivatives.
Bioorg Med Chem Lett 11: 2361-3 (2001)
Seoul National University
Structure-activity relationship studies of a bisbenzimidazole-based, Zn(2+)-dependent inhibitor of HCV NS3 serine protease.
Bioorg Med Chem Lett 11: 2355-9 (2001)
Bristol-Myers Squibb Pharmaceutical Research Institute
New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities.
Bioorg Med Chem Lett 11: 2345-9 (2001)
Solvay Pharma
The synthesis and tubulin binding activity of thiophene-based analogues of combretastatin A-4.
Bioorg Med Chem Lett 11: 2341-3 (2001)
Australian National University
Rational design and synthesis of novel 2,5-disubstituted cis- and trans-piperidine derivatives exhibiting differential activity for the dopamine transporter.
Bioorg Med Chem Lett 11: 2337-40 (2001)
Wayne State University
Monocharged inhibitors of mast cell tryptase derived from potent and selective dibasic inhibitors.
Bioorg Med Chem Lett 11: 2325-30 (2001)
Axys Pharmaceuticals
A novel phosphotyrosine mimetic 4'-carboxymethyloxy-3'-phosphonophenylalanine (Cpp): exploitation in the design of nonpeptide inhibitors of pp60(Src) SH2 domain.
Bioorg Med Chem Lett 11: 2319-23 (2001)
Ariad Pharmaceuticals
Metabolic stabilization of benzylidene ketal M(2) muscarinic receptor antagonists via halonaphthoic acid substitution.
Bioorg Med Chem Lett 11: 2311-4 (2001)
Schering-Plough Research Institute
Synthesis and purine receptor affinity of 6-oxopurine nucleosides and nucleotides containing (N)-methanocarba-pseudoribose rings.
Bioorg Med Chem Lett 11: 2295-300 (2001)
Niddk
Pyrazolecarboxamide human neuropeptide Y5 receptor ligands with in vivo antifeedant activity.
Bioorg Med Chem Lett 11: 2287-90 (2001)
The R. W. Johnson Pharmaceutical Research Institute
Aminopyrazoles with high affinity for the human neuropeptide Y5 receptor.
Bioorg Med Chem Lett 11: 2283-6 (2001)
The R. W. Johnson Pharmaceutical Research Institute
Design and synthesis of glycolic and mandelic acid derivatives as factor Xa inhibitors.
Bioorg Med Chem Lett 11: 2279-82 (2001)
Cor Therapeutics
Optimization of a screening lead for factor VIIa/TF.
Bioorg Med Chem Lett 11: 2253-6 (2001)
Axys Pharmaceuticals
Inhibitors of bacterial enoyl acyl carrier protein reductase (FabI): 2,9-disubstituted 1,2,3,4-tetrahydropyrido[3,4-b]indoles as potential antibacterial agents.
Bioorg Med Chem Lett 11: 2241-4 (2001)
Glaxosmithkline
Ellagitannins and hexahydroxydiphenoyl esters as inhibitors of vertebrate squalene epoxidase.
J Nat Prod 64: 1010-4 (2001)
University Of Shizuoka
Design and synthesis of celecoxib and rofecoxib analogues as selective cyclooxygenase-2 (COX-2) inhibitors: replacement of sulfonamide and methylsulfonyl pharmacophores by an azido bioisostere.
J Med Chem 44: 3039-42 (2001)
University Of Alberta
S(+)-4-(1-Phenylethylamino)quinazolines as inhibitors of human immunoglobulin E synthesis: potency is dictated by stereochemistry and atomic point charges at N-1.
J Med Chem 44: 3031-8 (2001)
Novartis Forschungsinstitut
Design, synthesis and pharmacological characterization of a potent radioiodinated and photoactivatable peptidic oxytocin antagonist.
J Med Chem 44: 3022-30 (2001)
University Of Montpellier
Identification of potent non-peptide somatostatin antagonists with sst(3) selectivity.
J Med Chem 44: 2990-3000 (2001)
Institut Henri Beaufour
5'-O-alkyl ethers of N,2-substituted adenosine derivatives: partial agonists for the adenosine A1 and A3 receptors.
J Med Chem 44: 2966-75 (2001)
Leiden/Amsterdam Center For Drug Research
Design and biological activity of (S)-4-(5-([1-(3-chlorobenzyl)-2-oxopyrrolidin-3-ylamino]methyl)imidazol-1-ylmethyl)benzonitrile, a 3-aminopyrrolidinone farnesyltransferase inhibitor with excellent cell potency.
J Med Chem 44: 2933-49 (2001)
Merck Research Laboratories
X-Ray crystal structures of Candida albicans dihydrofolate reductase: high resolution ternary complexes in which the dihydronicotinamide moiety of NADPH is displaced by an inhibitor.
J Med Chem 44: 2928-32 (2001)
Gsk
Design and synthesis of 4,5-diphenyl-4-isoxazolines: novel inhibitors of cyclooxygenase-2 with analgesic and antiinflammatory activity.
J Med Chem 44: 2921-7 (2001)
University Of Alberta
Discovery of potent antagonists of leukocyte function-associated antigen-1/intercellular adhesion molecule-1 interaction. 3. Amide (C-ring) structure-activity relationship and improvement of overall properties of arylthio cinnamides.
J Med Chem 44: 2913-20 (2001)
Abbott Laboratories
2-N-acylaminoalkylindoles: design and quantitative structure-activity relationship studies leading to MT2-selective melatonin antagonists.
J Med Chem 44: 2900-12 (2001)
Universit£
Synthesis, molecular modeling, and structure-activity relationship of benzophenone-based CAAX-peptidomimetic farnesyltransferase inhibitors.
J Med Chem 44: 2886-99 (2001)
Philipps-UniversitäT Marburg
Synthesis and characterization of non-steroidal ligands for the glucocorticoid receptor: selective quinoline derivatives with prednisolone-equivalent functional activity.
J Med Chem 44: 2879-85 (2001)
Abbott Laboratories
Utilization of a peptide lead for the discovery of a novel PTP1B-binding motif.
J Med Chem 44: 2869-78 (2001)
National Cancer Institute-Frederick
Structure-based design: potent inhibitors of human brain memapsin 2 (beta-secretase).
J Med Chem 44: 2865-8 (2001)
University Of Illinois At Chicago
Novel 4-piperidinopyridine inhibitors of oxidosqualene cyclase-lanosterol synthase derived by consideration of inhibitor pK(a).
Bioorg Med Chem Lett 11: 2213-6 (2001)
Astrazeneca
Identification of selective inhibitors of cyclin dependent kinase 4.
Bioorg Med Chem Lett 11: 2209-11 (2001)
Dupont Pharmaceuticals
The discovery of anthranilic acid-based MMP inhibitors. Part 2: SAR of the 5-position and P1(1) groups.
Bioorg Med Chem Lett 11: 2189-92 (2001)
Wyeth-Ayerst Research
Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists.
Bioorg Med Chem Lett 11: 2177-80 (2001)
Glaxosmithkline
Discovery of (R)-1-[2-hydroxy-3-(4-hydroxy-phenyl)-propyl]-4-(4-methyl-benzyl)-piperidin-4-ol: a novel NR1/2B subtype selective NMDA receptor antagonist.
Bioorg Med Chem Lett 11: 2173-6 (2001)
F. Hoffmann-La Roche
N,N-dibenzyl-N'-benzylidenehydrazines: potent competitive glucose-6-phosphatase catalytic enzyme inhibitors.
Bioorg Med Chem Lett 11: 2165-7 (2001)
Novo Nordisk
N-hydroxyformamide peptidomimetics as TACE/matrix metalloprotease inhibitors: oral activity via P1' isobutyl substitution.
Bioorg Med Chem Lett 11: 2147-51 (2001)
Glaxosmithkline
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. I: 2(S)-methyl piperazine as a key pharmacophore element.
Bioorg Med Chem Lett 11: 2143-6 (2001)
Schering-Plough Research Institute
5-HT(3)R binding of lerisetron: an interdisciplinary approach to drug-Receptor interactions.
Bioorg Med Chem Lett 11: 2133-6 (2001)
The University Of Louisiana At Monroe
Discovery of thioazepinone ligands for Src SH2: from non-specific to specific binding.
Bioorg Med Chem Lett 11: 2127-31 (2001)
Aventis
Stereoselective synthesis and antibacterial evaluation of 4-amido-isothiazolidinone oxides.
Bioorg Med Chem Lett 11: 2111-5 (2001)
Procter & Gamble Pharmaceuticals
Thrombin receptor (PAR-1) antagonists. Solid-phase synthesis of indole-based peptide mimetics by anchoring to a secondary amide.
Bioorg Med Chem Lett 11: 2105-9 (2001)
The R. W. Johnson Pharmaceutical Research Institute
Amino acid derived sulfonamide hydroxamates as inhibitors of procollagen C-proteinase: solid-phase synthesis of ornithine analogues.
Bioorg Med Chem Lett 11: 2085-8 (2001)
Roche Bioscience
Sar studies of piperidine-based analogues of cocaine. Part 3: oxadiazoles.
Bioorg Med Chem Lett 11: 2079-83 (2001)
Georgetown University Medical Center
Synthesis, antimalarial activity and inhibition of haem detoxification of novel bisquinolines.
Bioorg Med Chem Lett 11: 2075-7 (2001)
La Trobe University
Pyridopyrimidine analogues as novel adenosine kinase inhibitors.
Bioorg Med Chem Lett 11: 2071-4 (2001)
Abbott Laboratories
Structure-activity study and analgesic efficacy of amino acid derivatives as N-type calcium channel blockers.
Bioorg Med Chem Lett 11: 2067-70 (2001)
No Pharmaceutical
1,4-Disubstituted imidazoles are potential antibacterial agents functioning as inhibitors of enoyl acyl carrier protein reductase (FabI).
Bioorg Med Chem Lett 11: 2061-5 (2001)
Glaxosmithkline
The in vitro pharmacology of the beta-adrenergic receptor pet ligand (s)-fluorocarazolol reveals high affinity for cloned beta-adrenergic receptors and moderate affinity for the human 5-HT1A receptor.
Psychopharmacology (Berl) 157: 111-4 (2001)
Case Western Reserve University
Synthesis and pharmacological evaluation of dimeric muscarinic acetylcholine receptor agonists.
J Pharmacol Exp Ther 298: 1260-8 (2001)
University Of Melbourne
Identification of potent and selective neuropeptide Y Y(1) receptor agonists with orexigenic activity in vivo.
Mol Pharmacol 60: 534-40 (2001)
Schering-Plough Research Institute
Interaction of cations, anions, and weak base quinine with rat renal cation transporter rOCT2 compared with rOCT1.
Am J Physiol Renal Physiol 281: 454-68 (2001)
Institute Of Anatomy Of The Bayerische Julius-Maximilians-Universit£T
Inhibitors of human and rat testes microsomal 17beta-hydroxysteroid dehydrogenase (17beta-HSD) as potential agents for prostatic cancer.
J Enzym Inhib 16: 35-45 (2001)
Cardiff University
Potential of pyrazolooxadiazinone derivatives as serine protease inhibitors.
J Enzym Inhib 16: 15-34 (2001)
UniversitÀ
Photochemical synthesis of N-arylbenzophenanthridine selective estrogen receptor modulators (serms).
J Med Chem 44: 2857-60 (2001)
Eli Lilly
Synthesis and evaluation of 4-fluoro-8-substituted-2,3,4,5-tetrahydro-1H-2-benzazapines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.
J Med Chem 44: 2849-56 (2001)
University Of Kansas
Synthesis of and a comparative study on the inhibition of muscle and liver glycogen phosphorylases by epimeric pairs of d-gluco- and d-xylopyranosylidene-spiro-(thio)hydantoins and N-(d-glucopyranosyl) amides.
J Med Chem 44: 2843-8 (2001)
University Of Debrecen
Methylated analogues of methyl (R)-4-(3,4-dichlorophenylacetyl)- 3-(pyrrolidin-1-ylmethyl)piperazine-1-carboxylate (GR-89,696) as highly potent kappa-receptor agonists: stereoselective synthesis, opioid-receptor affinity, receptor selectivity, and functional studies.
J Med Chem 44: 2814-26 (2001)
Pharmazeutisches Institut Der Universit£T Freiburg
Development of serine protease inhibitors displaying a multicentered short (<2.3 A) hydrogen bond binding mode: inhibitors of urokinase-type plasminogen activator and factor Xa.
J Med Chem 44: 2753-71 (2001)
Axys Pharmaceuticals
Synthesis, mechanism of action, and antiviral activity of a new series of covalent mechanism-based inhibitors of S-adenosyl-L-homocysteine hydrolase.
J Med Chem 44: 2743-52 (2001)
Universit£
Fluorosulfonyl- and bis-(beta-chloroethyl)amino-phenylamino functionalized pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives: irreversible antagonists at the human A3 adenosine receptor and molecular modeling studies.
J Med Chem 44: 2735-42 (2001)
Università
6-Substituted-4-(3-bromophenylamino)quinazolines as putative irreversible inhibitors of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor (HER-2) tyrosine kinases with enhanced antitumor activity.
J Med Chem 44: 2719-34 (2001)
Wyeth-Ayerst Research
Design, synthesis, and structure-activity relationships of a series of 3-[2-(1-benzylpiperidin-4-yl)ethylamino]pyridazine derivatives as acetylcholinesterase inhibitors.
J Med Chem 44: 2707-18 (2001)
Universit£
Sorbitol dehydrogenase inhibitors (SDIs): a new potent, enantiomeric SDI, 4-[2-1R-hydroxy-ethyl)-pyrimidin-4-yl]piperazine-1-sulfonic acid dimethylamide.
J Med Chem 44: 2695-700 (2001)
Pfizer
Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213).
J Med Chem 44: 2691-4 (2001)
Friedrich-Alexander University
Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity.
J Med Chem 44: 2687-90 (2001)
Research Triangle Institute
Discovery of estrogen sulfotransferase inhibitors from a purine library screen.
J Med Chem 44: 2683-6 (2001)
University Of California
The first potent and selective inhibitors of the glycine transporter type 2.
J Med Chem 44: 2679-82 (2001)
Organon Laboratories
Synthesis of natural flutimide and analogous fully substituted pyrazine-2,6-diones, endonuclease inhibitors of influenza virus.
J Org Chem 66: 5504-16 (2001)
Merck Research Laboratories
HMG-CoA reductase inhibitors (statins) characterized as direct inhibitors of P-glycoprotein.
Pharm Res 18: 800-6 (2001)
Schering-Plough Research Institute
The complestatins as HIV-1 integrase inhibitors. Efficient isolation, structure elucidation, and inhibitory activities of isocomplestatin, chloropeptin I, new complestatins, A and B, and acid-hydrolysis products of chloropeptin I.
J Nat Prod 64: 874-82 (2001)
Merck Research Laboratories
Reduced amide bond peptidomimetics. (4S)-N-(4-amino-5-[aminoakyl]aminopentyl)-N'-nitroguanidines, potent and highly selective inhibitors of neuronal nitric oxide synthase.
J Med Chem 44: 2667-70 (2001)
Northwestern University
Design, synthesis, and structure-activity relationships of macrocyclic hydroxamic acids that inhibit tumor necrosis factor alpha release in vitro and in vivo.
J Med Chem 44: 2636-60 (2001)
Dupont Pharmaceuticals
Synthesis of 6- and 7- hydroxy-8-azabicyclo[3.2.1]octanes and their binding affinity for the dopamine and serotonin transporters.
J Med Chem 44: 2619-35 (2001)
Organix
Structure-activity studies of ground- and transition-state analogue inhibitors of cyclophilin.
J Med Chem 44: 2593-600 (2001)
Southern Methodist University
Design and synthesis of potent and selective alpha(4)beta(7) integrin antagonists.
J Med Chem 44: 2586-92 (2001)
Technische UniversitäT MüNchen
Disabling erbB receptors with rationally designed exocyclic mimetics of antibodies: structure-function analysis.
J Med Chem 44: 2565-74 (2001)
University Of Pennsylvania School Of Medicine
Structural studies on bioactive compounds. 34. Design, synthesis, and biological evaluation of triazenyl-substituted pyrimethamine inhibitors of Pneumocystis carinii dihydrofolate reductase.
J Med Chem 44: 2555-64 (2001)
University Of Nottingham
Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
J Med Chem 44: 2544-54 (2001)
Sapienza University Of Rome
Novel selective PDE4 inhibitors. 2. Synthesis and structure-activity relationships of 4-aryl-substituted cis-tetra- and cis-hexahydrophthalazinones.
J Med Chem 44: 2523-35 (2001)
Vrije Universiteit
Novel selective PDE4 inhibitors. 1. Synthesis, structure-activity relationships, and molecular modeling of 4-(3,4-dimethoxyphenyl)-2H-phthalazin-1-ones and analogues.
J Med Chem 44: 2511-22 (2001)
Vrije Universiteit
A rational approach to the design of selective substrates and potent nontransportable inhibitors of the excitatory amino acid transporter EAAC1 (EAAT3). new glutamate and aspartate analogues as potential neuroprotective agents.
J Med Chem 44: 2507-10 (2001)
TBA
Potent and selective carboxylic acid-based inhibitors of matrix metalloproteinases.
J Med Chem 44: 2499-502 (2001)
TBA
Physicochemical parameters responsible for the affinity of methotrexate analogs for rat canalicular multispecific organic anion transporter (cMOAT/MRP2).
Pharm Res 18: 579-86 (2001)
University Of Tokyo
GnRH antagonists: a new generation of long acting analogues incorporating p-ureido-phenylalanines at positions 5 and 6.
J Med Chem 44: 453-67 (2001)
Ferring Research Institute
Design, synthesis, and biological evaluation of a series of lavendustin A analogues that inhibit EGFR and Syk tyrosine kinases, as well as tubulin polymerization.
J Med Chem 44: 441-52 (2001)
Purdue University
Tyrosine kinase inhibitors. 18. 6-Substituted 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as soluble, irreversible inhibitors of the epidermal growth factor receptor.
J Med Chem 44: 429-40 (2001)
University Of Auckland
New 1-aryl-3-(4-arylpiperazin-1-yl)propane derivatives, with dual action at 5-HT1A serotonin receptors and serotonin transporter, as a new class of antidepressants.
J Med Chem 44: 418-28 (2001)
Universidad De Navarra
Behavioral approach to nondyskinetic dopamine antagonists: identification of seroquel.
J Med Chem 44: 372-89 (2001)
Astrazeneca Pharmaceuticals
Analogues of prazosin that bear a benextramine-related polyamine backbone exhibit different antagonism toward alpha1-adrenoreceptor subtypes.
J Med Chem 44: 362-71 (2001)
University Of Bologna
Synthesis and SAR of a new series of COX-2-selective inhibitors: pyrazolo[1,5-a]pyrimidines.
J Med Chem 44: 350-61 (2001)
J. Uriach & CíA.
Structure-activity relationships of pyridoxal phosphate derivatives as potent and selective antagonists of P2X1 receptors.
J Med Chem 44: 340-9 (2001)
National Institute Of Diabetes And Digestive And Kidney Diseases
3-Aryl[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: a new class of selective A1 adenosine receptor antagonists.
J Med Chem 44: 316-27 (2001)
Universit£
Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent.
J Med Chem 44: 305-15 (2001)
Universita' Degli Studi Di Salerno
Design of remarkably simple, yet potent urea-based inhibitors of glutamate carboxypeptidase II (NAALADase).
J Med Chem 44: 298-301 (2001)
TBA
New dermatological agents for the treatment of psoriasis.
J Med Chem 44: 281-97 (2001)
Allergan
Trace amines: identification of a family of mammalian G protein-coupled receptors.
Proc Natl Acad Sci U S A 98: 8966-71 (2001)
Synaptic Pharmaceutical
Cyclic imides as potent and selective alpha-1A adrenergic receptor antagonists.
Bioorg Med Chem Lett 11: 1959-62 (2001)
Merck
Spiro(indoline-3,4'-piperidine) growth hormone secretagogues as ghrelin mimetics.
Bioorg Med Chem Lett 11: 1955-7 (2001)
Merck Research Laboratories
Nicotinamide N-oxides as CXCR2 antagonists.
Bioorg Med Chem Lett 11: 1951-4 (2001)
Celltech R&D
Selectivity enhancement induced by substitution of non-natural analogues of arginine and lysine in arginine-based thrombin inhibitors.
Bioorg Med Chem Lett 11: 1947-50 (2001)
Medical University Of South Carolina
Synthesis and evaluation of novel quinolinones as HIV-1 reverse transcriptase inhibitors.
Bioorg Med Chem Lett 11: 1943-5 (2001)
Dupont Pharmaceuticals
2-Amino-4,6-diarylpyridines as novel ligands for the estrogen receptor.
Bioorg Med Chem Lett 11: 1939-42 (2001)
Glaxo Wellcome Research And Development
alpha-Ketocarboxylic acid-based inhibitors of protein tyrosine phosphatases.
Bioorg Med Chem Lett 11: 1935-8 (2001)
Brown University
Introduction of alkynyl chains on C-8 of adenosine led to very selective antagonists of the A(3) adenosine receptor.
Bioorg Med Chem Lett 11: 1931-4 (2001)
Universit£
1-(Arylpiperazinylamidoalkyl)-pyrimidones: orally active inhibitors of lipoprotein-associated phospholipase A(2).
Bioorg Med Chem Lett 11: 1925-9 (2001)
Glaxosmithkline
Synthesis of N(1)-substituted analogues of (2R,4R)-4-amino-pyrrolidine-2,4-dicarboxylic acid as agonists, partial agonists, and antagonists of group II metabotropic glutamate receptors.
Bioorg Med Chem Lett 11: 1919-24 (2001)
Georgetown University Medical Center
Studies leading to the identification of ZD1839 (IRESSA): an orally active, selective epidermal growth factor receptor tyrosine kinase inhibitor targeted to the treatment of cancer.
Bioorg Med Chem Lett 11: 1911-4 (2001)
Astrazeneca
1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor.
Bioorg Med Chem Lett 11: 1907-10 (2001)
Glaxosmithkline
3-Arylpiperidines as potentiators of existing antibacterial agents.
Bioorg Med Chem Lett 11: 1903-6 (2001)
Pharmacia
Development of specific CXCR4 inhibitors possessing high selectivity indexes as well as complete stability in serum based on an anti-HIV peptide T140.
Bioorg Med Chem Lett 11: 1897-902 (2001)
Kyoto University
Macrocyclization in the design of a conformationally constrained Grb2 SH2 domain inhibitor.
Bioorg Med Chem Lett 11: 1889-92 (2001)
National Institutes Of Health
Studies towards the next generation of antidepressants. Part 1: Indolylcyclohexylamines as potent serotonin reuptake inhibitors.
Bioorg Med Chem Lett 11: 1885-8 (2001)
Wyeth-Ayerst Research Laboratories
Phytoestrogens from the roots of Polygonum cuspidatum (Polygonaceae): structure-requirement of hydroxyanthraquinones for estrogenic activity.
Bioorg Med Chem Lett 11: 1839-42 (2001)
Kyoto Pharmaceutical University
Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 1.
Bioorg Med Chem Lett 11: 1833-7 (2001)
Nippon Roche Research Center
Nitrobenzene compounds inhibit expression of VCAM-1.
Bioorg Med Chem Lett 11: 1823-7 (2001)
Atherogenics
Evaluation of amino acid-based linkers in potent macrocyclic inhibitors of farnesyl-protein transferase.
Bioorg Med Chem Lett 11: 1817-21 (2001)
Merck Research Laboratories
Inhibition of fucosyltransferase V by a GDP-Azasugar.
Bioorg Med Chem Lett 11: 1809-11 (2001)
Technische Universit£T Berlin
Novel tricyclic benzothiazolo[2,3-c]thiadiazine antagonists of the platelet ADP receptor (P2Y(12)).
Bioorg Med Chem Lett 11: 1805-8 (2001)
Cor Therapeutics
Development of potent and selective factor Xa inhibitors.
Bioorg Med Chem Lett 11: 1797-800 (2001)
Axys Pharmaceuticals
SL651498: an anxioselective compound with functional selectivity for alpha2- and alpha3-containing gamma-aminobutyric acid(A) (GABA(A)) receptors.
J Pharmacol Exp Ther 298: 753-68 (2001)
Sanofi Synthelabo
S33005, a novel ligand at both serotonin and norepinephrine transporters: I. Receptor binding, electrophysiological, and neurochemical profile in comparison with venlafaxine, reboxetine, citalopram, and clomipramine.
J Pharmacol Exp Ther 298: 565-80 (2001)
Institut De Recherches Servier
[3H]LY341495 binding to group II metabotropic glutamate receptors in rat brain.
J Pharmacol Exp Ther 298: 453-60 (2001)
Eli Lilly
Prevention of allergic inflammation by a novel prostaglandin receptor antagonist, S-5751.
J Pharmacol Exp Ther 298: 411-9 (2001)
Shionogi
Evaluation of the interaction of loratadine and desloratadine with P-glycoprotein.
Drug Metab Dispos 29: 1080-3 (2001)
Schering-Plough Research Institute
Design and synthesis of a highly selective EP4-receptor agonist. Part 2: 5-thia and 9beta-haloPG derivatives with improved stability.
Bioorg Med Chem Lett 11: 2033-5 (2001)
Minase Research Institute
Design and synthesis of a highly selective EP4-receptor agonist. Part 1: 3,7-dithiaPG derivatives with high selectivity.
Bioorg Med Chem Lett 11: 2029-31 (2001)
Minase Research Institute
Design and synthesis of a highly selective EP2-receptor agonist.
Bioorg Med Chem Lett 11: 2025-8 (2001)
Minase Research Institute
Substituted 4-phenyl-2-(phenylcarboxamido)-1,3-thiazole derivatives as antagonists for the adenosine A(1) receptor.
Bioorg Med Chem Lett 11: 2017-9 (2001)
Leiden/Amsterdam Center For Drug Research
alpha(v)beta(3) Antagonists based on a central thiophene scaffold.
Bioorg Med Chem Lett 11: 2011-5 (2001)
Aventis Pharma Deutschland
Discovery and SAR of org 24598-a selective glycine uptake inhibitor.
Bioorg Med Chem Lett 11: 2007-9 (2001)
Organon Research And Development Group
Synthesis of N-alkyl substituted indolocarbazoles as potent inhibitors of human cytomegalovirus replication.
Bioorg Med Chem Lett 11: 1993-5 (2001)
Glaxosmithkline
The development of new carboxylic acid-based MMP inhibitors derived from a cyclohexylglycine scaffold.
Bioorg Med Chem Lett 11: 1975-9 (2001)
Procter And Gamble Pharmaceuticals
P-glycoprotein interactions of nefazodone and trazodone in cell culture.
J Clin Pharmacol 41: 708-14 (2001)
Tufts University School Of Medicine
Hexosaminidase inhibitors as new drug candidates for the therapy of osteoarthritis.
Chem Biol 8: 701-11 (2001)
The Scripps Research Institute
Bisubstrate ketone analogues as serotonin N-acetyltransferase inhibitors.
J Med Chem 44: 2479-85 (2001)
Johns Hopkins University School Of Medicine
Peptide folding induces high and selective affinity of a linear and small beta-peptide to the human somatostatin receptor 4.
J Med Chem 44: 2460-8 (2001)
Eth Zurich
Nonpeptidic, monocharged, cell permeable ligands for the p56lck SH2 domain.
J Med Chem 44: 2421-31 (2001)
Boehringer Ingelheim (Canada)
Volume learning algorithm artificial neural networks for 3D QSAR studies.
J Med Chem 44: 2411-20 (2001)
Institute Of Bioorganic & Petroleum Chemistry
Phenylpiperazinylalkylamino substituted pyridazinones as potent alpha(1) adrenoceptor antagonists.
J Med Chem 44: 2403-10 (2001)
Istituto Chimico Farmaceutico E Tossicologico
Design, synthesis, computational prediction, and biological evaluation of ester soft drugs as inhibitors of dihydrofolate reductase from Pneumocystis carinii.
J Med Chem 44: 2391-402 (2001)
Uppsala University
Novel C-terminus modifications of the Dmt-Tic motif: a new class of dipeptide analogues showing altered pharmacological profiles toward the opioid receptors.
J Med Chem 44: 2387-90 (2001)
Astrazeneca R&D Montreal
Reversible carnitine palmitoyltransferase inhibitors with broad chemical diversity as potential antidiabetic agents.
J Med Chem 44: 2383-6 (2001)
Sigma Tau Pharmaceutical Industries
The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound.
Eur J Pharmacol 423: 71-83 (2001)
Janssen Research Foundation
Functional characterization of the human multidrug transporter, ABCG2, expressed in insect cells.
Biochem Biophys Res Commun 285: 111-7 (2001)
Hungarian Academy Of Sciences
Natural product-based anti-HIV drug discovery and development facilitated by the NCI developmental therapeutics program.
J Nat Prod 64: 265-77 (2001)
National Cancer Institute
Isoaurostatin, a novel topoisomerase inhibitor produced by Thermomonospora alba.
J Nat Prod 64: 204-7 (2001)
Kumamoto University
Synthesis and structure-activity relationships of trisubstituted phenyl urea derivatives as neuropeptide Y5 receptor antagonists.
J Med Chem 44: 2344-56 (2001)
Amgen
A new concept for multidimensional selection of ligand conformations (MultiSelect) and multidimensional scoring (MultiScore) of protein-ligand binding affinities.
J Med Chem 44: 2333-43 (2001)
The Royal Danish School Of Pharmacy
4-Hydroxy-5,6-dihydropyrones as inhibitors of HIV protease: the effect of heterocyclic substituents at C-6 on antiviral potency and pharmacokinetic parameters.
J Med Chem 44: 2319-32 (2001)
Pfizer
Enantioselective syntheses of potent retinoid X receptor ligands: differential biological activities of individual antipodes.
J Med Chem 44: 2298-303 (2001)
Allergan
Novel N-(arylalkyl)indol-3-ylglyoxylylamides targeted as ligands of the benzodiazepine receptor: synthesis, biological evaluation, and molecular modeling analysis of the structure-activity relationships.
J Med Chem 44: 2286-97 (2001)
Università
Utilization of an intramolecular hydrogen bond to increase the CNS penetration of an NK(1) receptor antagonist.
J Med Chem 44: 2276-85 (2001)
Cambridge University Forvie Site
Isomerization of (Z,Z) to (E,E)1-bromo-2,5-bis-(3-hydroxycarbonyl-4-hydroxy)styrylbenzene in strong base: probes for amyloid plaques in the brain.
J Med Chem 44: 2270-5 (2001)
University Of Pennsylvania
Characterization of organic anion transport inhibitors using cells stably expressing human organic anion transporters.
Eur J Pharmacol 419: 113-20 (2001)
Kyorin University
Carbonic anhydrase inhibitors: 4-sulfamoyl-benzenecarboxamides and 4-chloro-3-sulfamoyl-benzenecarboxamides with strong topical antiglaucoma properties.
Bioorg Med Chem Lett 11: 1787-91 (2001)
Universit£
Novel and potent tacrine-related hetero- and homobivalent ligands for acetylcholinesterase and butyrylcholinesterase.
Bioorg Med Chem Lett 11: 1779-82 (2001)
Universita Degli Studi Di Siena
Significance of hydrogen bonding at the S(1)' subsite of calpain I.
Bioorg Med Chem Lett 11: 1753-5 (2001)
The University Of Tennessee
Piperazinyl benzamidines: synthesis and affinity for the delta opioid receptor.
Bioorg Med Chem Lett 11: 1741-3 (2001)
R. W. Johnson Pharmaceutical Research Institute
Isoindolines: a new series of potent and selective endothelin-A receptor antagonists.
Bioorg Med Chem Lett 11: 1737-40 (2001)
Novartis Institute For Biomedical Research
Potent nonpeptide GnRH receptor antagonists derived from substituted indole-5-carboxamides and -acetamides bearing a pyridine side-chain terminus.
Bioorg Med Chem Lett 11: 1727-31 (2001)
Merck Research Laboratories
Substituted indole-5-carboxamides and -acetamides as potent nonpeptide GnRH receptor antagonists.
Bioorg Med Chem Lett 11: 1723-6 (2001)
Merck Research Laboratories
3-Carboxamido analogues of morphine and naltrexone. synthesis and opioid receptor binding properties.
Bioorg Med Chem Lett 11: 1717-21 (2001)
Pharmacia
Biphenyls as surrogates of the steroidal backbone. Part 2: discovery of a novel family of non-steroidal 5-alpha-reductase inhibitors.
Bioorg Med Chem Lett 11: 1713-6 (2001)
Aventis
Total synthesis of human chymase inhibitor methyllinderone and structure--activity relationships of its derivatives.
Bioorg Med Chem Lett 11: 1695-7 (2001)
Shionogi
Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones.
Bioorg Med Chem Lett 11: 1691-4 (2001)
Shionogi
Synthesis of substituted 5[H]phenanthridin-6-ones as potent poly(ADP-ribose)polymerase-1 (PARP1) inhibitors.
Bioorg Med Chem Lett 11: 1687-90 (2001)
Guilford Pharmaceuticals
Novel sulfonate derivatives: potent antimitotic agents.
Bioorg Med Chem Lett 11: 1671-3 (2001)
Abbott Laboratories
Selective inhibition of Src SH2 by a novel thiol-targeting tricarbonyl-modified inhibitor and mechanistic analysis by (1)H/(13)C NMR spectroscopy.
Bioorg Med Chem Lett 11: 1665-9 (2001)
Ariad Pharmaceuticals
[3H]MFZ 2-12: a novel radioligand for the dopamine transporter.
Bioorg Med Chem Lett 11: 1659-61 (2001)
National Institute On Drug Abuse-Intramural Research Program
Nucleoside analogues as highly potent and selective inhibitors of herpes simplex virus thymidine kinase.
Bioorg Med Chem Lett 11: 1655-8 (2001)
Roche Discovery Welwyn
Expedited discovery of second generation NK-1 antagonists: identification of a nonbasic aryloxy substituent.
Bioorg Med Chem Lett 11: 1643-6 (2001)
Eli Lilly
Quinoline-4-acetamides as sPLA(2) inhibitors.
Bioorg Med Chem Lett 11: 1639-41 (2001)
Peking University
Dibasic inhibitors of human mast cell tryptase. Part 3: identification of a series of potent and selective inhibitors containing the benzamidine functionality.
Bioorg Med Chem Lett 11: 1629-33 (2001)
Axys Pharmaceuticals
Novel heteroaryl replacements of aromatic 3-tetrafluoroethoxy substituents in trifluoro-3-(tertiaryamino)-2-propanols as potent inhibitors of cholesteryl ester transfer protein.
Bioorg Med Chem Lett 11: 1625-8 (2001)
Pharmacia
Steroidal alkaloids from the leaves of Sarcococca coriacea of Nepalese origin.
J Nat Prod 64: 842-4 (2001)
Tribhuvan University
Cox-2 inhibitory effects of naturally occurring and modified fatty acids.
J Nat Prod 64: 745-9 (2001)
Uppsala University
Synthesis and evaluation of GGPP geometric isomers: divergent substrate specificities of FTase and GGTase I.
Bioorg Med Chem Lett 11: 1605-8 (2001)
Wayne State University
Synthesis of novel sialylmimetics as biological probes.
Bioorg Med Chem Lett 11: 1587-90 (2001)
Monash University (Parkville Campus)
An unhydrolyzable analogue of N-(4-hydroxyphenyl)retinamide. synthesis and preliminary biological studies.
Bioorg Med Chem Lett 11: 1583-6 (2001)
The Ohio State University
Phenylethanolamine N-methyltransferase kinetics: bovine versus recombinant human enzyme.
Bioorg Med Chem Lett 11: 1579-82 (2001)
University Of Kansas
Bioisosteric determinants for subtype selectivity of ligands for heteromeric GABA(A) receptors.
Bioorg Med Chem Lett 11: 1573-7 (2001)
The Royal Danish School Of Pharmacy
New probes of the agonist binding site of metabotropic glutamate receptors.
Bioorg Med Chem Lett 11: 1569-72 (2001)
Universit£
Cyclooxygenase-inhibitory and antioxidant constituents of the aerial parts of Antirhea acutata.
Bioorg Med Chem Lett 11: 1565-8 (2001)
University Of Illinois At Chicago
Discovery and characterization of the potent, selective and orally bioavailable MMP inhibitor ABT-770.
Bioorg Med Chem Lett 11: 1557-60 (2001)
Abbott Laboratories
Biaryl ether retrohydroxamates as potent, long-lived, orally bioavailable MMP inhibitors.
Bioorg Med Chem Lett 11: 1553-6 (2001)
Abbott Laboratories
Amidino benzimidazole inhibitors of bacterial two-component systems.
Bioorg Med Chem Lett 11: 1545-8 (2001)
The R. W. Johnson Pharmaceutical Research Institute
alpha-Keto heterocycle inhibitors of fatty acid amide hydrolase: carbonyl group modification and alpha-substitution.
Bioorg Med Chem Lett 11: 1517-20 (2001)
The Scripps Research Institute
Aromatic inhibitors of dehydroquinate synthase: synthesis, evaluation and implications for gallic acid biosynthesis.
Bioorg Med Chem Lett 11: 1493-6 (2001)
Michigan State University
Structure-based design and in-parallel synthesis of inhibitors of AmpC beta-lactamase.
Chem Biol 8: 593-611 (2001)
Northwestern University
Evidence for a new G protein-coupled cannabinoid receptor in mouse brain.
Mol Pharmacol 60: 155-63 (2001)
Virginia Commonwealth University
The peptide YY-preferring receptor mediating inhibition of small intestinal secretion is a peripheral Y(2) receptor: pharmacological evidence and molecular cloning.
Mol Pharmacol 60: 124-34 (2001)
U410
Characterization of the efflux transport of 17beta-estradiol-D-17beta-glucuronide from the brain across the blood-brain barrier.
J Pharmacol Exp Ther 298: 316-22 (2001)
The University Of Tokyo
Pharmacological characterization of ZD6021: a novel, orally active antagonist of the tachykinin receptors.
J Pharmacol Exp Ther 298: 307-15 (2001)
Astrazeneca Pharmaceuticals
Rabbit alpha2-adrenoceptors: both platelets and adipocytes have alpha2A-pharmacology.
J Pharmacol Exp Ther 298: 219-25 (2001)
Glaxosmithkline
Methadone inhibits rhodamine123 transport in Caco-2 cells.
Drug Metab Dispos 29: 954-6 (2001)
Tufts University School Of Medicine
Protease inhibitors: synthesis of a series of bacterial collagenase inhibitors of the sulfonyl amino acyl hydroxamate type.
J Med Chem 44: 2253-8 (2001)
The University Of Western Australia
Characterization of melanocortin NDP-MSH agonist peptide fragments at the mouse central and peripheral melanocortin receptors.
J Med Chem 44: 2247-52 (2001)
University Of Florida
Potent somatostatin undecapeptide agonists selective for somatostatin receptor 1 (sst1).
J Med Chem 44: 2238-46 (2001)
Salk Institute
Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2-exo-2-(2'-substituted 5'-pyridinyl)-7-azabicyclo[2.2.1]heptanes. Epibatidine analogues.
J Med Chem 44: 2229-37 (2001)
Research Triangle Institute
5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1)receptor antagonists: structure-activity relationship studies on the substituent at N2-position.
J Med Chem 44: 2219-28 (2001)
Instituto De Qu£Mica M£Dica (Csic)
Novel, potent, and selective phosphodiesterase 5 inhibitors: synthesis and biological activities of a series of 4-aryl-1-isoquinolinone derivatives.
J Med Chem 44: 2204-18 (2001)
Tanabe Seiyaku
Combinatorial synthesis of cholesterol ester transfer protein-mRNA ligands and screening by nondenaturating gel-electrophoresis.
J Med Chem 44: 2172-7 (2001)
Johann Wolfgang Goethe-Universit£T Frankfurt/Main
Synthesis of novel gamma-aminobutyric acid (GABA) uptake inhibitors. 5.(1) Preparation and structure-activity studies of tricyclic analogues of known GABA uptake inhibitors.
J Med Chem 44: 2152-63 (2001)
Novo Nordisk
Discovery of 4-amino-5-(3-bromophenyl)-7-(6-morpholino-pyridin-3-yl)pyrido[2,3-d]pyrimidine, an orally active, non-nucleoside adenosine kinase inhibitor..
J Med Chem 44: 2133-8 (2001)
Abbott Laboratories
Synthesis, biological evaluation, and pharmacophore generation of new pyridazinone derivatives with affinity toward alpha(1)- and alpha(2)-adrenoceptors.
J Med Chem 44: 2118-32 (2001)
Universit£
Development of potent non-carbohydrate imidazole-based small molecule selectin inhibitors with antiinflammatory activity.
J Med Chem 44: 2094-107 (2001)
Ontogen
Adenosine analogues as selective inhibitors of glyceraldehyde-3-phosphate dehydrogenase of Trypanosomatidae via structure-based drug design.
J Med Chem 44: 2080-93 (2001)
University Of Washington
Transformation of a kappa-opioid receptor antagonist to a kappa-agonist by transfer of a guanidinium group from the 5'- to 6'-position of naltrindole.
J Med Chem 44: 2073-9 (2001)
University Of Minnesota
3-(4-aroyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides, a new class of synthetic histone deacetylase inhibitors.
J Med Chem 44: 2069-72 (2001)
Università
Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists.
J Med Chem 44: 2061-4 (2001)
Eli Lilly
Secretase targets for Alzheimer's disease: identification and therapeutic potential.
J Med Chem 44: 2039-60 (2001)
Harvard Medical School
A functional assay for quantitation of the apparent affinities of ligands of P-glycoprotein in Caco-2 cells.
Pharm Res 18: 171-6 (2001)
The University Of Kansas
Identification and characterization of a second melanin-concentrating hormone receptor, MCH-2R.
Proc Natl Acad Sci U S A 98: 7564-9 (2001)
Merck Research Laboratories
Powerful probes for glycosidases: novel, fluorescently tagged glycosidase inhibitors.
Bioorg Med Chem Lett 11: 1339-42 (2001)
Institut FüR Biochemie Der Technischen UniversitäT Graz
Ring-Constrained (N)-methanocarba nucleosides as adenosine receptor agonists: independent 5'-uronamide and 2'-deoxy modifications.
Bioorg Med Chem Lett 11: 1333-7 (2001)
Niddk
Design, synthesis and enzymatic activity of highly selective human mitochondrial thymidine kinase inhibitors.
Bioorg Med Chem Lett 11: 1329-32 (2001)
Universit£
Thiazole analogues of the NSAID indomethacin as selective COX-2 inhibitors.
Bioorg Med Chem Lett 11: 1325-8 (2001)
Abbott Laboratories
Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic?
Bioorg Med Chem Lett 11: 1313-6 (2001)
Ucb Pharma
Structure-activity relationship investigations of a potent and selective benzodiazepine oxytocin antagonist.
Bioorg Med Chem Lett 11: 1301-5 (2001)
Glaxosmithkline
Identification of a potent and selective oxytocin antagonist, from screening a fully encoded differential release combinatorial chemical library.
Bioorg Med Chem Lett 11: 1297-300 (2001)
Glaxosmithkline
Spirocyclic nonpeptide glycoprotein IIb-IIIa antagonists. Part 2: design of potent antagonists containing the 3-azaspiro[5.5]undecanes.
Bioorg Med Chem Lett 11: 1293-6 (2001)
Cor Therapeutics
Spirocyclic nonpeptide glycoprotein IIb-IIIa antagonists. Part 1: design of potent and specific 3,9-diazaspiro[5.5]undecanes.
Bioorg Med Chem Lett 11: 1289-92 (2001)
Cor Therapeutics
Synthesis and biological evaluations of condensed pyridine and condensed pyrimidine-based HMG-CoA reductase inhibitors.
Bioorg Med Chem Lett 11: 1285-8 (2001)
Central Research Institute
Synthesis and evaluation of a difluoromethylene analogue of sphingomyelin as an inhibitor of sphingomyelinase.
Bioorg Med Chem Lett 11: 1277-80 (2001)
Tokyo University Of Pharmacy & Life Science
Synthesis and antifungal activities of novel 1,3-beta-D-glucan synthase inhibitors. Part 2.
Bioorg Med Chem Lett 11: 1273-6 (2001)
Nippon Roche Research Center
Diaryl ether inhibitors of farnesyl-protein transferase.
Bioorg Med Chem Lett 11: 1257-60 (2001)
Merck Research Laboratories
Potent and selective nonpeptide inhibitors of caspases 3 and 7.
J Med Chem 44: 2015-26 (2001)
Glaxosmithkline
Synthesis, antifolate, and antitumor activities of classical and nonclassical 2-amino-4-oxo-5-substituted-pyrrolo[2,3-d]pyrimidines.
J Med Chem 44: 1993-2003 (2001)
Duquesne University
Structure-activity studies for a novel series of bicyclic substituted hexahydrobenz[e]isoindole alpha1A adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia.
J Med Chem 44: 1971-85 (2001)
Abbott Laboratories
Solid-phase synthesis of a nonpeptide RGD mimetic library: new selective alphavbeta3 integrin antagonists.
J Med Chem 44: 1938-50 (2001)
Technische UniversitäT MüNchen
Soluble 2-substituted aminopyrido[2,3-d]pyrimidin-7-yl ureas. Structure-activity relationships against selected tyrosine kinases and exploration of in vitro and in vivo anticancer activity.
J Med Chem 44: 1915-26 (2001)
Pfizer
Radioiodinated styrylbenzenes and thioflavins as probes for amyloid aggregates.
J Med Chem 44: 1905-14 (2001)
University Of Pennsylvania
An optimized protein kinase C activating diacylglycerol combining high binding affinity (Ki) with reduced lipophilicity (log P).
J Med Chem 44: 1892-904 (2001)
National Cancer Institute-Frederick
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
J Med Chem 44: 1866-82 (2001)
Glaxosmithkline
Identification of a putative binding site for [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide)thymine (TSAO) derivatives at the p51-p66 interface of HIV-1 reverse transcriptase.
J Med Chem 44: 1853-65 (2001)
Universidad De Alcal£
2-(2-Oxo-1,4-dihydro-2H-quinazolin-3-yl)- and 2-(2,2-dioxo-1,4-dihydro-2H-2lambda6-benzo[1,2,6]thiadiazin-3-yl)-N-hydroxy-acetamides as potent and selective peptide deformylase inhibitors.
J Med Chem 44: 1847-52 (2001)
F. Hoffmann-La Roche
Arylsulphonyl hydroxamic acids: potent and selective matrix metalloproteinase inhibitors.
Bioorg Med Chem Lett 11: 1465-8 (2001)
Celltech-Chiroscience
Fine Tuning of physico-chemical parameters to optimise a new series of novobiocin analogues.
Bioorg Med Chem Lett 11: 1461-4 (2001)
Aventis Pharma
Discovery of potent and selective phenylalanine derived CCR3 receptor antagonists. Part 2.
Bioorg Med Chem Lett 11: 1445-50 (2001)
Smithkline Beecham Pharmaceuticals
Discovery of potent and selective phenylalanine derived CCR3 antagonists. Part 1.
Bioorg Med Chem Lett 11: 1441-4 (2001)
Smithkline Beecham Pharmaceuticals
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 1: discovery of the pyrrolidine scaffold and determination of its stereochemical requirements.
Bioorg Med Chem Lett 11: 1437-40 (2001)
Merck Research Laboratories
Discovery of a nuclease-resistant, non-natural dinucleotide that inhibits HIV-1 integrase.
Bioorg Med Chem Lett 11: 1433-5 (2001)
The University Of Iowa
Effect of zinc ion on the inhibition of carboxypeptidase A by imidazole-bearing substrate analogues.
Bioorg Med Chem Lett 11: 1425-7 (2001)
Pohang University Of Science And Technology
Aryloxy substituted N-arylpiperazinones as dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
Bioorg Med Chem Lett 11: 1411-5 (2001)
Merck Research Laboratories
MEK (MAPKK) inhibitors. Part 2: structure-activity relationships of 4-anilino-3-cyano-6,7-dialkoxyquinolines.
Bioorg Med Chem Lett 11: 1407-10 (2001)
Wyeth-Ayerst Research
Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2.
Bioorg Med Chem Lett 11: 1401-5 (2001)
Research Biomet. Glaxo Wellcome Medicines Research Centre
Structure-activity relationships of phenylcyclohexene and biphenyl antitubulin compounds against plant and mammalian cells.
Bioorg Med Chem Lett 11: 1393-6 (2001)
Rohm And Haas
4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors.
Bioorg Med Chem Lett 11: 1389-92 (2001)
Dupont Pharmaceuticals
Structure-based design, synthesis and SAR of a novel series of thiopheneamidine urokinase plasminogen activator inhibitors.
Bioorg Med Chem Lett 11: 1379-82 (2001)
3-Dimensional Pharmaceuticals
Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands.
Bioorg Med Chem Lett 11: 1375-7 (2001)
Columbia University College Of Physicians And Surgeons
5,5-Diaryl-2-amino-4-pentenoates as novel, potent, and selective glycine transporter type-2 reuptake inhibitors.
Bioorg Med Chem Lett 11: 1371-3 (2001)
Nps Pharmaceuticals
Identification of novel potent hydroxamic acid inhibitors of peptidyl deformylase and the importance of the hydroxamic acid functionality on inhibition.
Bioorg Med Chem Lett 11: 1355-8 (2001)
Pharmacia
Synthesis and antiviral activities of the major metabolites of the HIV protease inhibitor ABT-378 (Lopinavir).
Bioorg Med Chem Lett 11: 1351-3 (2001)
Abbott Laboratories
Coumarins isolated from Angelica gigas inhibit acetylcholinesterase: structure-activity relationships.
J Nat Prod 64: 683-5 (2001)
Seoul National University
New sesquiterpene derivatives from the sponge Dysidea species with a selective inhibitor profile against human phospholipase A2 and other leukocyte functions.
J Nat Prod 64: 612-5 (2001)
Università
Antimalarial, cytotoxic, and antifungal alkaloids from Duguetia hadrantha.
J Nat Prod 64: 559-62 (2001)
University Of Mississippi
Antiparkinsonian agent piribedil displays antagonist properties at native, rat, and cloned, human alpha(2)-adrenoceptors: cellular and functional characterization.
J Pharmacol Exp Ther 297: 876-87 (2001)
Institut De Recherches Servier
Synthesis and structure-activity relationships of naphthamides as dopamine D3 receptor ligands.
J Med Chem 44: 1815-26 (2001)
Wake Forest University School Of Medicine
Enantioselective syntheses of dopaminergic (R)- and (S)-benzyltetrahydroisoquinolines.
J Med Chem 44: 1794-801 (2001)
Universidad De Valencia
Potent reversible inhibitors of the protein tyrosine phosphatase CD45.
J Med Chem 44: 1777-93 (2001)
Astrazeneca Pharmaceuticals
Synthesis and biological evaluation of purine-containing butenolides.
J Med Chem 44: 1749-57 (2001)
Academia Sinica
Homology modeling using multiple molecular dynamics simulations and docking studies of the human androgen receptor ligand binding domain bound to testosterone and nonsteroidal ligands.
J Med Chem 44: 1729-40 (2001)
The University Of Tennessee Health Science Center
Discovery of novel aldose reductase inhibitors using a protein structure-based approach: 3D-database search followed by design and synthesis.
J Med Chem 44: 1718-28 (2001)
Sankyo
Structural basis of binding of high-affinity ligands to protein kinase C: prediction of the binding modes through a new molecular dynamics method and evaluation by site-directed mutagenesis.
J Med Chem 44: 1690-701 (2001)
Georgetown University Medical Center
Stepwise modulation of neurokinin-3 and neurokinin-2 receptor affinity and selectivity in quinoline tachykinin receptor antagonists.
J Med Chem 44: 1675-89 (2001)
Smithkline Beecham Pharmaceuticals
Development of a pharmacophore model for histamine H3 receptor antagonists, using the newly developed molecular modeling program SLATE.
J Med Chem 44: 1666-74 (2001)
De Novo Pharmaceuticals
Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens.
J Med Chem 44: 1654-7 (2001)
Wyeth-Ayerst Research
Recent developments in the biology and medicinal chemistry of potassium channel modulators: update from a decade of progress.
J Med Chem 44: 1627-53 (2001)
Abbott Laboratories
Neuronal nicotinic acetylcholine receptor binding affinities of boron-containing nicotine analogues.
Bioorg Med Chem Lett 11: 1245-8 (2001)
University Of Kentucky
Design and pharmacology of quinuclidine derivatives as M2-selective muscarinic receptor ligands.
Bioorg Med Chem Lett 11: 1241-3 (2001)
University Of Mainz
2-Aryl indole NK1 receptor antagonists: optimisation of the 2-aryl ring and the indole nitrogen substituent.
Bioorg Med Chem Lett 11: 1237-40 (2001)
Merck Sharp And Dohme Research Laboratories
2-Aryl indole NK1 receptor antagonists: optimisation of indole substitution.
Bioorg Med Chem Lett 11: 1233-6 (2001)
The Neuroscience Research Centre
Influence of the terminal amide fragment geometry in some 3-arylideneindolin-2(1H)-ones on their 5-HT1A/5-HT2A receptor activity.
Bioorg Med Chem Lett 11: 1229-31 (2001)
Polish Academy Of Sciences
Identification of a subtype selective human PPARalpha agonist through parallel-array synthesis.
Bioorg Med Chem Lett 11: 1225-7 (2001)
Glaxosmithkline
Discovery of a novel CCR3 selective antagonist.
Bioorg Med Chem Lett 11: 1219-23 (2001)
Banyu Tsukuba Research Institute
Syntheses and evaluation of quinoline derivatives as novel retinoic acid receptor alpha antagonists.
Bioorg Med Chem Lett 11: 1215-8 (2001)
Eisai
Design and synthesis of 2-oxo-imidazolidine-4-carboxylic acid hydroxyamides as potent matrix metalloproteinase-13 inhibitors.
Bioorg Med Chem Lett 11: 1211-3 (2001)
Pfizer
Convergent synthesis of potent peptide inhibitors of the Grb2-SH2 domain by palladium catalyzed coupling of a terminal alkyne.
Bioorg Med Chem Lett 11: 1201-3 (2001)
Novartis Pharma
Quinazolines as cyclin dependent kinase inhibitors.
Bioorg Med Chem Lett 11: 1157-60 (2001)
Dupont Pharmaceuticals
Inhibition of neuronal nitric oxide synthase by 7-methoxyindazole and related substituted indazoles.
Bioorg Med Chem Lett 11: 1153-6 (2001)
Université
Conformational analysis of tandospirone in aqueous solution: lead evolution of potent dopamine D4 receptor ligands.
Bioorg Med Chem Lett 11: 1141-4 (2001)
Sumitomo Pharmaceuticals
Glycosidase inhibition by cyclic sulfonium compounds.
Bioorg Med Chem Lett 11: 1137-9 (2001)
Graduate School Of Bioscience And Biotechnology
Binding of dimeric aminoglycosides to the HIV-1 rev responsive element (RRE) RNA construct.
Bioorg Med Chem Lett 11: 1127-31 (2001)
Purdue University
Phenoxypyrimidine inhibitors of p38alpha kinase: synthesis and statistical evaluation of the p38 inhibitory potencies of a series of 1-(piperidin-4-yl)-4-(4-fluorophenyl)-5-(2-phenoxypyrimidin-4-yl) imidazoles.
Bioorg Med Chem Lett 11: 1123-6 (2001)
Glaxosmithkline
Two novel and potent 3-[(o-methoxyphenyl)piperazinylethyl]-5-phenylthien.
Bioorg Med Chem Lett 11: 1119-21 (2001)
Abbott Laboratories
Pharmacophore-based discovery of 3,4-disubstituted pyrrolidines as a novel class of monoamine transporter inhibitors.
Bioorg Med Chem Lett 11: 1113-8 (2001)
Georgetown University Medical Center
Design and synthesis of a new sialyl Lewis X mimetic: how selective are the selectin receptors?
Bioorg Med Chem Lett 11: 1109-12 (2001)
Universit£
Structural basis for inhibition promiscuity of dual specific thrombin and factor Xa blood coagulation inhibitors.
Structure 9: 29-37 (2001)
Boehringer Ingelheim Pharma
Small molecule peptidomimetics containing a novel phosphotyrosine bioisostere inhibit protein tyrosine phosphatase 1B and augment insulin action.
Biochemistry 40: 5642-54 (2001)
Pharmacia
Combinatorial lead optimization of a neuropeptide FF antagonist.
J Med Chem 44: 1623-6 (2001)
University Of Florida
Pharmacological and behavioral analysis of the effects of some bivalent ligand-based monoamine reuptake inhibitors.
J Med Chem 44: 1615-22 (2001)
Georgetown University Medical Center
3-(4-Fluoropiperidin-3-yl)-2-phenylindoles as high affinity, selective, and orally bioavailable h5-HT(2A) receptor antagonists.
J Med Chem 44: 1603-14 (2001)
Merck Sharp And Dohme Research Laboratories
Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues.
J Med Chem 44: 1594-602 (2001)
Life Science Research Center
Synthesis and biological evaluation of pyrrolinic isosteres of rilmenidine. Discovery of cis-/trans-dicyclopropylmethyl-(4,5-dimethyl-4,5-dihydro-3H-pyrrol-2-yl)-amine (LNP 509), an I1 imidazoline receptor selective ligand with hypotensive activity.
J Med Chem 44: 1588-93 (2001)
Universit£
Computational analysis of PKA-balanol interactions.
J Med Chem 44: 1530-9 (2001)
University Of California At San Diego
Synthesis of 2beta-acyl-3beta-(substituted naphthyl)-8-azabicyclo[3.2.1]octanes and their binding affinities at dopamine and serotonin transport sites.
J Med Chem 44: 1509-15 (2001)
State University Of New York
Design, synthesis, and proposed active site binding analysis of monocyclic 2-azetidinone inhibitors of prostate specific antigen.
J Med Chem 44: 1491-508 (2001)
University Of Oxford
Highly selective and potent neuropeptide Y (NPY) Y1 receptor antagonists based on [Pro(30), Tyr(32), Leu(34)]NPY(28-36)-NH2 (BW1911U90).
J Med Chem 44: 1479-82 (2001)
University Of Cincinnati And Va Medical Centers
Allyl and propargyl substituted penam sulfones as versatile intermediates toward the syntheses of new beta-lactamase inhibitors.
Bioorg Med Chem Lett 11: 997-1000 (2001)
Wyeth-Ayerst Research
Novel non-peptide ligands for the somatostatin sst3 receptor.
Bioorg Med Chem Lett 11: 991-5 (2001)
Institut Henri Beaufour
New oxadiazolidinedione derivatives as potent and selective human beta3 agonists.
Bioorg Med Chem Lett 11: 981-4 (2001)
Wyeth-Ayerst Research
Discovery and SAR of diarylsulfide cyclopropylamide LFA-1/ICAM-1 interaction antagonists.
Bioorg Med Chem Lett 11: 973-6 (2001)
Abbott Laboratories
Novel 5,5-disubstitutedpyrimidine-2,4,6-triones as selective MMP inhibitors.
Bioorg Med Chem Lett 11: 969-72 (2001)
Roche Research Center
Vanilloid and isovanilloid analogues as inhibitors of methionyl-tRNA and isoleucyl-tRNA synthetases.
Bioorg Med Chem Lett 11: 965-8 (2001)
Seoul National University
Ester and hydroxamate analogues of methionyl and isoleucyl adenylates as inhibitors of methionyl-tRNA and isoleucyl-tRNA synthetases.
Bioorg Med Chem Lett 11: 961-4 (2001)
Seoul National University
Rational design, synthesis, and biological evaluation of rigid pyrrolidone analogues as potential inhibitors of prostate cancer cell growth.
Bioorg Med Chem Lett 11: 955-9 (2001)
Georgetotwn University
Synthesis and structure-activity relationships of guanine analogues as phosphodiesterase 7 (PDE7) inhibitors.
Bioorg Med Chem Lett 11: 1081-3 (2001)
Celltech R&D
Heterocyclic derivatives of 2-(3,5-dimethylphenyl)tryptamine as GnRH receptor antagonists.
Bioorg Med Chem Lett 11: 1077-80 (2001)
Merck Research Laboratories
2-(3,5-Dimethylphenyl)tryptamine derivatives that bind to the GnRH receptor.
Bioorg Med Chem Lett 11: 1073-6 (2001)
Merck Research Laboratories
1,2,5-Thiadiazole derivatives are potent and selective ligands at human 5-HT1A receptors.
Bioorg Med Chem Lett 11: 1069-71 (2001)
Wyeth-Ayerst Research
Design, synthesis and stability of N-acyloxymethyl- and N-aminocarbonyloxymethyl-2-azetidinones as human leukocyte elastase inhibitors.
Bioorg Med Chem Lett 11: 1065-8 (2001)
Ineti
Novel, lipophilic derivatives of 2,5-dideoxy-2,5-imino-D-mannitol (DMDP) are powerful beta-glucosidase inhibitors.
Bioorg Med Chem Lett 11: 1063-4 (2001)
Technische UniversitäT Graz
In vitro metabolism considerations, including activity testing of metabolites, in the discovery and selection of the COX-2 inhibitor etoricoxib (MK-0663).
Bioorg Med Chem Lett 11: 1059-62 (2001)
Merck Frosst Centre For Therapeutic Research
Synthesis and structure-activity studies of side-chain derivatized arylhydantoins for investigation as androgen receptor radioligands.
Bioorg Med Chem Lett 11: 1045-7 (2001)
The University Of Michigan Medical School
2-Acylimino-3H-thiazoline derivatives: a novel template for platelet GPIIb/IIIa receptor antagonists.
Bioorg Med Chem Lett 11: 1031-5 (2001)
Taisho Pharmaceutical
Thienopyridines: nitric oxide synthase inhibitors with potent in vivo activity.
Bioorg Med Chem Lett 11: 1027-30 (2001)
Astrazeneca R&D Charnwood
3,4-Dihydro-1-isoquinolinamines: a novel class of nitric oxide synthase inhibitors with a range of isoform selectivity and potency.
Bioorg Med Chem Lett 11: 1023-6 (2001)
Astrazeneca R&D Charnwood
Structure determination and comparison of BM567, a sulfonylurea, with terbogrel, two compounds with dual action, thromboxane receptor antagonism and thromboxane synthase inhibition.
Bioorg Med Chem Lett 11: 1019-22 (2001)
FacultéS Universitaires N.D. De La Paix
Heterocycle-based MMP inhibitors with P2' substituents.
Bioorg Med Chem Lett 11: 1009-13 (2001)
Procter And Gamble Pharmaceuticals
Microxine, a new cdc2 kinase inhibitor from the Australian marine sponge Microxina species.
J Nat Prod 64: 525-6 (2001)
Harbor Branch Oceanographic Institution
Identification of thyroid hormone transporters in humans: different molecules are involved in a tissue-specific manner.
Endocrinology 142: 2005-12 (2001)
Tohoku University School Of Medicine
Highly potent and subtype selective ligands derived by N-methyl scan of a somatostatin antagonist.
J Med Chem 44: 1305-11 (2001)
Tulane University Health Sciences Center
Synthesis, structure-activity relationships, and pharmacokinetic profiles of nonpeptidic difluoromethylene ketones as novel inhibitors of human chymase.
J Med Chem 44: 1297-304 (2001)
Welfide
Synthesis, structure-activity relationships, and pharmacokinetic profiles of nonpeptidic alpha-keto heterocycles as novel inhibitors of human chymase.
J Med Chem 44: 1286-96 (2001)
Welfide
Development of orally active nonpeptidic inhibitors of human neutrophil elastase.
J Med Chem 44: 1268-85 (2001)
Cortech
Angular methoxy-substituted furo- and pyranoquinolinones as blockers of the voltage-gated potassium channel Kv1.3.
J Med Chem 44: 1249-56 (2001)
University Of Kiel
Acyl substitution at the ortho position of anilides enhances oral bioavailability of thiophene sulfonamides: TBC3214, an ETA selective endothelin antagonist.
J Med Chem 44: 1211-6 (2001)
Texas Biotechnology
Novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intracellular adhesion molecule-1 interaction. 2. Mechanism of inhibition and structure-based improvement of pharmaceutical properties.
J Med Chem 44: 1202-10 (2001)
Abbott Laboratories
Design, synthesis, and structural analysis of influenza neuraminidase inhibitors containing pyrrolidine cores.
J Med Chem 44: 1192-201 (2001)
Abbott Laboratories
Discovery of an orally active non-peptide fibrinogen receptor antagonist based on the hydantoin scaffold.
J Med Chem 44: 1158-76 (2001)
Aventis Pharma
Comparative molecular field analysis of dopamine D4 receptor antagonists including 3-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 113), 3-[4-(4-chlorophenyl)piperazin-1-ylmethyl]-1H-pyrrolo-[2,3-b]pyridine (L-745,870), and clozapine.
J Med Chem 44: 1151-7 (2001)
Friedrich-Alexander University
Mapping and fitting the peripheral benzodiazepine receptor binding site by carboxamide derivatives. Comparison of different approaches to quantitative ligand-receptor interaction modeling.
J Med Chem 44: 1134-50 (2001)
Universit£
Neonicotinoid insecticides: molecular features conferring selectivity for insect versus mammalian nicotinic receptors.
J Agric Food Chem 48: 6016-24 (2000)
University Of California
Effect of N-alkyl and N-alkenyl substituents in noroxymorphindole, 17-substituted-6,7-dehydro-4,5alpha-epoxy-3,14-dihydroxy-6,7:2',3'-indolomorphinans, on opioid receptor affinity, selectivity, and efficacy.
J Med Chem 44: 1471-4 (2001)
National Institute Of Diabetes And Digestive And Kidney Diseases
(4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists.
J Med Chem 44: 1456-66 (2001)
Wyeth-Ayerst Research
Discovery of novel N-phenylglycine derivatives as potent and selective beta(3)-adrenoceptor agonists for the treatment of frequent urination and urinary incontinence.
J Med Chem 44: 1436-45 (2001)
Kissei Pharmaceutical
Design, synthesis, and discovery of a novel CCR1 antagonist.
J Med Chem 44: 1429-35 (2001)
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
N-Methyl scan of somatostatin octapeptide agonists produces interesting effects on receptor subtype specificity.
J Med Chem 44: 1416-21 (2001)
Tulane University Health Sciences Center
Azepanone-based inhibitors of human and rat cathepsin K.
J Med Chem 44: 1380-95 (2001)
Glaxosmithkline
Development of potent truncated glucagon antagonists.
J Med Chem 44: 1372-9 (2001)
University Of Arizona
Structure-based approach for the discovery of bis-benzamidines as novel inhibitors of matriptase.
J Med Chem 44: 1349-55 (2001)
Georgetown University Medical Center
Atropisomeric derivatives of 2',6'-disubstituted (R)-11-phenylaporphine: selective serotonin 5-HT(7) receptor antagonists.
J Med Chem 44: 1337-40 (2001)
Uppsala University
Indenopyrazoles as novel cyclin dependent kinase (CDK) inhibitors.
J Med Chem 44: 1334-6 (2001)
Dupont Pharmaceuticals
The endothelin antagonist bosentan inhibits the canalicular bile salt export pump: a potential mechanism for hepatic adverse reactions.
Clin Pharmacol Ther 69: 223-31 (2001)
University Of Zurich
Modulation of multidrug resistance protein 1 (MRP1/ABCC1) transport and atpase activities by interaction with dietary flavonoids.
Mol Pharmacol 59: 1171-80 (2001)
Queen'S University
Charged amino acids in the transmembrane domains are involved in the determination of the substrate specificity of rat Mrp2.
Mol Pharmacol 59: 1077-85 (2001)
The University Of Tokyo
BAY36-7620: a potent non-competitive mGlu1 receptor antagonist with inverse agonist activity.
Mol Pharmacol 59: 965-73 (2001)
Upr 9023
The vnd/NK-2 homeodomain: thermodynamics of reversible unfolding and DNA binding for wild-type and with residue replacements H52R and H52R/T56W in helix III.
Biochemistry 40: 4923-31 (2001)
National Institutes Of Health
Pharmacological properties of (2R)-N-[1-(6-aminopyridin-2-ylmethyl)piperidin-4-yl]-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxy-2-phenylacetamide: a novel mucarinic antagonist with M(2)-sparing antagonistic activity.
J Pharmacol Exp Ther 297: 790-7 (2001)
Banyu Pharmaceutical
Molecular and pharmacological characterization of muscarinic receptor subtypes in a rat parotid gland cell line: comparison with native parotid gland.
J Pharmacol Exp Ther 297: 718-26 (2001)
Creighton University
Pharmacological characterization of KUR-1246, a selective uterine relaxant.
J Pharmacol Exp Ther 297: 666-71 (2001)
Kissei Pharmaceutical
Enantiospecific synthesis and pharmacological evaluation of a series of super-potent, conformationally restricted 5-HT(2A/2C) receptor agonists.
J Med Chem 44: 1003-10 (2001)
Purdue University
Discovery of inhibitors of cell adhesion molecule expression in human endothelial cells. 1. Selective inhibition of ICAM-1 and E-selectin expression.
J Med Chem 44: 988-1002 (2001)
Abbott Laboratories
Factors influencing agonist potency and selectivity for the opioid delta receptor are revealed in structure-activity relationship studies of the 4-[(N-substituted-4-piperidinyl)arylamino]-N,N-diethylbenzamides.
J Med Chem 44: 972-87 (2001)
Research Triangle Institute
Structure-activity relationship studies of 4-[2-(diphenylmethoxy)ethyl]-1-benzylpiperidine derivatives and their N-analogues: evaluation of O-and N-analogues and their binding to monoamine transporters.
J Med Chem 44: 937-48 (2001)
Wayne State University
A potent, nonpeptidyl 1H-quinolone antagonist for the gonadotropin-releasing hormone receptor.
J Med Chem 44: 917-22 (2001)
Merck Research Laboratories
Pharmacophore analysis of the nuclear oxysterol receptor LXRalpha.
J Med Chem 44: 886-97 (2001)
Dartmouth College
Alpha(2) adrenoceptor agonists as potential analgesic agents. 3. Imidazolylmethylthiophenes.
J Med Chem 44: 863-72 (2001)
The R. W. Johnson Pharmaceutical Research Institute
Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the"address" recognition locus.
J Med Chem 44: 857-62 (2001)
University Of Minnesota
A novel series of highly potent benzimidazole-based microsomal triglyceride transfer protein inhibitors.
J Med Chem 44: 851-6 (2001)
The Bristol-Myers Squibb Pharmaceutical Research Institute
Investigations into migraine pathogenesis: time course for effects of m-CPP, BW723C86 or glyceryl trinitrate on appearance of Fos-like immunoreactivity in rat trigeminal nucleus caudalis (TNC).
Cephalalgia 21: 46-52 (2001)
Roche Bioscience
Flexible estrogen receptor modulators: design, synthesis, and antagonistic effects in human MCF-7 breast cancer cells.
J Med Chem 44: 1072-84 (2001)
Trinity College
Development of new carboxylic acid-based MMP inhibitors derived from functionalized propargylglycines.
J Med Chem 44: 1060-71 (2001)
Procter And Gamble Pharmaceuticals
Estimation of binding affinities for selective thrombin inhibitors via Monte Carlo simulations.
J Med Chem 44: 1043-50 (2001)
Yale University
Molecular models of N-benzyladriamycin-14-valerate (AD 198) in complex with the phorbol ester-binding C1b domain of protein kinase C-delta.
J Med Chem 44: 1028-34 (2001)
University Of Tennessee College Of Medicine
Substituted pyrazolopyridines as potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction.
J Med Chem 44: 1025-7 (2001)
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery and optimization of a novel series of thrombin receptor (par-1) antagonists: potent, selective peptide mimetics based on indole and indazole templates.
J Med Chem 44: 1021-4 (2001)
The R. W. Johnson Pharmaceutical Research Institute
Covalently induced activation of the delta opioid receptor by a fluorogenic affinity label, 7'-(phthalaldehydecarboxamido)naltrindole (PNTI).
J Med Chem 44: 1017-20 (2001)
University Of Minnesota
Different antagonist binding properties of human and rat histamine H3 receptors.
Bioorg Med Chem Lett 11: 951-4 (2001)
Freie UniversitäT Berlin
Selective delta-opioid receptor ligands: potential PET ligands based on naltrindole.
Bioorg Med Chem Lett 11: 939-43 (2001)
University Of Bristol
Synthesis and biological evaluation of a sialyl Lewis X mimic with significantly improved E-selectin inhibition.
Bioorg Med Chem Lett 11: 923-5 (2001)
Novartis Pharma
Synthesis of thiophene-2-carboxamidines containing 2-aminothiazoles and their biological evaluation as urokinase inhibitors.
Bioorg Med Chem Lett 11: 915-8 (2001)
3-Dimensional Pharmaceuticals
LY294002-geldanamycin heterodimers as selective inhibitors of the PI3K and PI3K-related family.
Bioorg Med Chem Lett 11: 909-13 (2001)
Department Of Molecular Oncogenesis
Acid dissociation constant, a potential physicochemical factor in the inhibition of the enzyme estrone sulfatase (ES).
Bioorg Med Chem Lett 11: 899-902 (2001)
Kingston University
The discovery of a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase--GW311616A a development candidate.
Bioorg Med Chem Lett 11: 895-8 (2001)
Glaxowellcome Medicines Research Centre
Design and synthesis of ether analogues as potent and selective M2 muscarinic receptor antagonists.
Bioorg Med Chem Lett 11: 891-4 (2001)
Schering-Plough Research Institute
Cis- and trans-N-benzyl-octahydrobenzo[g]quinolines. Adrenergic and dopaminergic activity studies.
Bioorg Med Chem Lett 11: 883-6 (2001)
University Of Crete
Synthesis and structure-activity relationships of 1-phenylpyrazoles as xanthine oxidase inhibitors.
Bioorg Med Chem Lett 11: 879-82 (2001)
Welfide
Novel sulfonate analogues of combretastatin A-4: potent antimitotic agents.
Bioorg Med Chem Lett 11: 871-4 (2001)
Abbott Laboratories
2-Arylindole-3-acetamides: FPP-competitive inhibitors of farnesyl protein transferase.
Bioorg Med Chem Lett 11: 865-9 (2001)
Merck Research Laboratories
A novel serine protease inhibition motif involving a multi-centered short hydrogen bonding network at the active site.
J Mol Biol 307: 1451-86 (2001)
Axys Pharmaceuticals
A novel inhibitor of the mammalian peptide transporter PEPT1.
Biochemistry 40: 4454-8 (2001)
Martin-Luther-University Halle-Wittenberg
Expression cloning of a Na+-independent aromatic amino acid transporter with structural similarity to H+/monocarboxylate transporters.
J Biol Chem 276: 17221-8 (2001)
Kyorin University
Cheilanthane sesterterpenes, protein kinase inhibitors, from a marine sponge of the genus Ircinia.
J Nat Prod 64: 300-3 (2001)
Astrazeneca R&D Griffith University
7-Pyrrolidinyl- and 7-piperidinyl-5-aryl-pyrrolo[2,3-d]pyrimidines--potent inhibitors of the tyrosine kinase c-Src.
Bioorg Med Chem Lett 11: 853-6 (2001)
Novartis Pharma Research
7-Alkyl- and 7-cycloalkyl-5-aryl-pyrrolo[2,3-d]pyrimidines--potent inhibitors of the tyrosine kinase c-Src.
Bioorg Med Chem Lett 11: 849-52 (2001)
Novartis Pharma Research
N-Aminoindoline derivatives as inhibitors of 5-lipoxygenase.
Bioorg Med Chem Lett 11: 845-8 (2001)
Université
Novel inhibitors of the enzyme estrone sulfatase (ES).
Bioorg Med Chem Lett 11: 841-4 (2001)
Kingston University
Effects of two-carbon bridge region methoxylation of benztropine: discovery of novel chiral ligands for the dopamine transporter.
Bioorg Med Chem Lett 11: 823-7 (2001)
Universit£
Spatial requirements of the antagonist binding site of the NK2 receptor.
Bioorg Med Chem Lett 11: 819-22 (2001)
University Of Leeds
Synthesis and use of FSCPX, an irreversible adenosine A1 antagonist, as a 'receptor knock-down' tool.
Bioorg Med Chem Lett 11: 815-8 (2001)
Vrije Universiteit
Discovery of zoniporide: a potent and selective sodium-hydrogen exchanger type 1 (NHE-1) inhibitor with high aqueous solubility.
Bioorg Med Chem Lett 11: 803-7 (2001)
Pfizer
A novel fluorinated tryptamine with highly potent serotonin 5-HT1A receptor agonist properties.
Bioorg Med Chem Lett 11: 793-5 (2001)
Purdue University
Phenylcyclohexene and phenylcyclohexadiene substituted compounds having retinoid antagonist activity.
Bioorg Med Chem Lett 11: 765-8 (2001)
Allergan
Peptidomimetic inhibitors of protein farnesyltransferase show potent antimalarial activity.
Bioorg Med Chem Lett 11: 761-4 (2001)
Yale University
2,4-Thiazolidinediones as potent and selective human beta3 agonists.
Bioorg Med Chem Lett 11: 757-60 (2001)
Wyeth-Ayerst Research
A robust GTP-induced shift in alpha(2)-adrenoceptor agonist affinity in tissue sections from rat brain.
J Neurosci Methods 105: 159-66 (2001)
University Of Nebraska
Dynorphin A analogs containing a conformationally constrained phenylalanine derivative in position 4: reversal of preferred stereochemistry for opioid receptor affinity and discrimination of kappa vs. delta receptors.
Chirality 13: 125-9 (2001)
University Of Maryland
Structure-activity relationship on the human EP3 prostanoid receptor by use of solid-support chemistry.
Bioorg Med Chem Lett 11: 747-9 (2001)
Merck Frosst Canada
Synthesis of substituted imidazopyrazines as ligands for the human somatostatin receptor subtype 5.
Bioorg Med Chem Lett 11: 741-5 (2001)
Institut Henri Beaufour
Structure-activity analysis of truncated orexin-A analogues at the orexin-1 receptor.
Bioorg Med Chem Lett 11: 737-40 (2001)
Smithkline Beecham Pharmaceuticals
The design of phenylglycine containing benzamidine carboxamides as potent and selective inhibitors of factor Xa.
Bioorg Med Chem Lett 11: 733-6 (2001)
Prosthetics Molecular Design
The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities.
Bioorg Med Chem Lett 11: 723-8 (2001)
Kyoto University
The C4 hydroxyl group of phorbol esters is not necessary for protein kinase C binding.
Bioorg Med Chem Lett 11: 719-22 (2001)
Kyoto University
Potent synthetic inhibitors of tyrosyl tRNA synthetase derived from C-pyranosyl analogues of SB-219383.
Bioorg Med Chem Lett 11: 715-8 (2001)
Glaxosmithkline
Synthetic analogues of SB-219383. Novel C-glycosyl peptides as inhibitors of tyrosyl tRNA synthetase.
Bioorg Med Chem Lett 11: 711-4 (2001)
Glaxosmithkline
Design of non-peptide CCK2 and NK1 peptidomimetics using 1-(2-nitrophenyl)thiosemicarbazide as a novel common scaffold.
Bioorg Med Chem Lett 11: 705-9 (2001)
Novartis Institute For Medical Sciences
The identification of a potent, water soluble inhibitor of lipoprotein-associated phospholipase A2.
Bioorg Med Chem Lett 11: 701-4 (2001)
Glaxosmithkline
RPR203494 a pyrimidine analogue of the p38 inhibitor RPR200765A with an improved in vitro potency.
Bioorg Med Chem Lett 11: 693-6 (2001)
Aventis Pharma
Design and synthesis of novel 2,3-dihydro-1H-isoindoles with high affinity and selectivity for the dopamine D3 receptor.
Bioorg Med Chem Lett 11: 685-8 (2001)
Smithkline Beecham Pharmaceuticals
Gamma-lactone-Functionalized antitumoral acetogenins are the most potent inhibitors of mitochondrial complex I.
Bioorg Med Chem Lett 11: 681-4 (2001)
Universidad De Valencia
Sialidase inhibitors related to zanamivir. Further SAR studies of 4-amino-4H-pyran-2-carboxylic acid-6-propylamides.
Bioorg Med Chem Lett 11: 669-73 (2001)
Glaxowellcome Medicines Research Centre
Synthesis, modelling and NK1 antagonist evaluation of a non-rigid cyclopropane-containing analogue of CP-99,994.
Bioorg Med Chem Lett 11: 659-61 (2001)
Laboratoire De Chimie ThéRapeutique Associé
Influence of chain length and N-alkylation on the selective serotonin receptor ligand 9-(aminomethyl)-9,10-dihydroanthracene.
Bioorg Med Chem Lett 11: 655-8 (2001)
Virginia Commonwealth University
Importance of the C28-C38 hydrophobic domain of okadaic acid for potent inhibition of protein serine-threonine phosphatases 1 and 2A.
Bioorg Med Chem Lett 11: 647-9 (2001)
University Of Minnesota
Synthesis and SAR of benzamidine factor Xa inhibitors containing a vicinally-substituted heterocyclic core.
Bioorg Med Chem Lett 11: 641-5 (2001)
Dupont Pharmaceuticals
3-Anilino-4-arylmaleimides: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3).
Bioorg Med Chem Lett 11: 635-9 (2001)
Smithkline Beecham Pharmaceuticals
Synthesis and structure-activity relationships of 5-substituted pyridine analogues of 3.
Bioorg Med Chem Lett 11: 631-3 (2001)
Abbott Laboratories
Chemoenzymatic synthesis of functionalized cyclohexylglycines and alpha-methylcyclohexylglycines via Kazmaier-Claisen rearrangement.
Bioorg Med Chem Lett 11: 627-9 (2001)
University Of Florida
8-Carboxamidocyclazocine analogues: redefining the structure-activity relationships of 2,6-methano-3-benzazocines.
Bioorg Med Chem Lett 11: 623-6 (2001)
Rensselaer Polytechnic Institute
Synthesis and biological activities of potential metabolites of the non-nucleoside reverse transcriptase inhibitor efavirenz.
Bioorg Med Chem Lett 11: 619-22 (2001)
Dupont Pharmaceuticals
Syntheses and evaluation of pyrido[2,3-dlpyrimidine-2,4-diones as PDE 4 inhibitors.
Bioorg Med Chem Lett 11: 611-4 (2001)
Korea Institute Of Science And Technology
Syntheses and biological activities of a novel group of steroidal derived inhibitors for human Cdc25A protein phosphatase.
J Med Chem 44: 834-48 (2001)
Georgia Institute Of Technology
Synthesis and Src kinase inhibitory activity of a series of 4-phenylamino-3-quinolinecarbonitriles.
J Med Chem 44: 822-33 (2001)
Wyeth-Ayerst Research
Potential antidepressants displayed combined alpha(2)-adrenoceptor antagonist and monoamine uptake inhibitor properties.
J Med Chem 44: 787-805 (2001)
Institut De Recherches Servier
Thiazole and thiadiazole analogues as a novel class of adenosine receptor antagonists.
J Med Chem 44: 749-62 (2001)
Vrije Universiteit
Cyclic ketone inhibitors of the cysteine protease cathepsin K.
J Med Chem 44: 725-36 (2001)
Gsk
Correlation of anti-HIV activity with anion spacing in a series of cosalane analogues with extended polycarboxylate pharmacophores.
J Med Chem 44: 703-14 (2001)
Purdue University
Discovery of 4-[3-(trans-3-dimethylaminocyclobutyl)-1H-indol-5-ylmethyl]-(4S)-oxazolidin-2-one (4991W93), a 5HT(1B/1D) receptor partial agonist and a potent inhibitor of electrically induced plasma extravasation.
J Med Chem 44: 681-93 (2001)
Glaxowellcome
A new class of nonsteroidal aromatase inhibitors: design and synthesis of chromone and xanthone derivatives and inhibition of the P450 enzymes aromatase and 17 alpha-hydroxylase/C17,20-lyase.
J Med Chem 44: 672-80 (2001)
University Of Bologna
X-Ray structure of citrate bound to Src SH2 leads to a high-affinity, bone-targeted Src SH2 inhibitor.
J Med Chem 44: 660-3 (2001)
Ariad Pharmaceuticals
Perspectives in animal health: old targets and new opportunities.
J Med Chem 44: 641-59 (2001)
Merck Research Laboratories
Zebra finch CB1 cannabinoid receptor: pharmacology and in vivo and in vitro effects of activation.
J Pharmacol Exp Ther 297: 189-97 (2001)
Florida State University
Carrier-mediated hepatobiliary transport of a novel antifolate, N-[4-[(2,4-dianninopteridine-6-yl)methyl]-3,4-dihydro-2H-1,4-benzothiazin-7-yl]carbonyl-L-homoglutamic acid, in rats.
Drug Metab Dispos 29: 394-400 (2001)
University Of Tokyo
Characterization of bile acid transport mediated by multidrug resistance associated protein 2 and bile salt export pump.
Biochim Biophys Acta 1511: 7-16 (2001)
The University Of Tokyo
Inhibitory effects of CYP3A4 substrates and their metabolites on P-glycoprotein-mediated transport.
Eur J Pharm Sci 12: 505-13 (2001)
Kanazawa University
New 5-HT1A receptor agonists possessing 1,4-benzoxazepine scaffold exhibit highly potent anti-ischemic effects.
Bioorg Med Chem Lett 11: 595-8 (2001)
Suntory Biomedical Research
Aminoglycoside antibiotics, neamine and its derivatives as potent inhibitors for the RNA-protein interactions derived from HIV-1 activators.
Bioorg Med Chem Lett 11: 591-4 (2001)
Graduate School Of Bioscience And Biotechnology
Pyrrolidine inhibitors of human cytosolic phospholipase A2. Part 2: synthesis of potent and crystallized 4-triphenylmethylthio derivative 'pyrrophenone'.
Bioorg Med Chem Lett 11: 587-90 (2001)
Shionogi
Development of novel telomerase inhibitors based on a bisindole unit.
Bioorg Med Chem Lett 11: 583-5 (2001)
Kyushu University
Carbonic anhydrase inhibitors: synthesis of sulfonamides incorporating dtpa tails and of their zinc complexes with powerful topical antiglaucoma properties.
Bioorg Med Chem Lett 11: 575-82 (2001)
Universit£
Discovery of potent and selective succinyl hydroxamate inhibitors of matrix metalloprotease-3 (stromelysin-1).
Bioorg Med Chem Lett 11: 571-4 (2001)
Pfizer
Selectivity of inhibition of matrix metalloproteases MMP-3 and MMP-2 by succinyl hydroxamates and their carboxylic acid analogues is dependent on P3' group chirality.
Bioorg Med Chem Lett 11: 567-70 (2001)
Pfizer
Exploring the relationship between binding modes of 9-(aminomethyl)-9,10-dihydroanthracene and cyproheptadine analogues at the 5-HT2A serotonin receptor.
Bioorg Med Chem Lett 11: 563-6 (2001)
Virginia Commonwealth University
Pimarane cyclooxygenase 2 (COX-2) inhibitor and its structure-activity relationship.
Bioorg Med Chem Lett 11: 559-62 (2001)
Seoul National University
Peptoids as endothelin receptor antagonists.
Bioorg Med Chem Lett 11: 555-7 (2001)
Ranbaxy Laboratories
A series of quinoline analogues as potent inhibitors of C. albicans prolyl tRNA synthetase.
Bioorg Med Chem Lett 11: 541-4 (2001)
Cubist Pharmaceuticals
Oxo-piperazine derivatives of N-arylpiperazinones as inhibitors of farnesyltransferase.
Bioorg Med Chem Lett 11: 537-40 (2001)
Merck Research Laboratories
Synthesis of analogues of the O-beta-D-ribofuranosyl nucleoside moiety of liposidomycins. Part 1: contribution of the amino group and the uracil moiety upon the inhibition of MraY.
Bioorg Med Chem Lett 11: 529-31 (2001)
Aventis Pharma
Anti-HIV activity of aromatic and heterocyclic thiazolyl thiourea compounds.
Bioorg Med Chem Lett 11: 523-8 (2001)
Institute
SAR studies of novel 5-substituted 2-arylindoles as nonpeptidyl GnRH receptor antagonists.
Bioorg Med Chem Lett 11: 515-7 (2001)
Merck Research Laboratories
Initial structure-activity relationship of a novel class of nonpeptidyl GnRH receptor antagonists: 2-arylindoles.
Bioorg Med Chem Lett 11: 509-13 (2001)
Merck Research Laboratories
Identification and characterization of a potential ischemia-selective N-methyl-D-aspartate (NMDA) receptor ion-channel blocker, CNS 5788.
Bioorg Med Chem Lett 11: 501-4 (2001)
Cambridge Neuroscience
Synthesis of substituted 4(Z)-(methoxyimino)pentyl-1-piperidines as dual NK1/NK2 inhibitors.
Bioorg Med Chem Lett 11: 491-4 (2001)
Schering-Plough Research Institute
Synthesis and monoamine transporter affinity of 3beta-(4-(2-pyrrolyl)phenyl)-8-azabicycl.
Bioorg Med Chem Lett 11: 487-9 (2001)
State University Of New York
Beta-D-glycosylamidines: potent, selective, and easily accessible 1-glycosidase inhibitors.
Bioorg Med Chem Lett 11: 467-70 (2001)
Kyoto University
Synthesis of sialyl Lewis(x) mimics. Modifications of the 6-position of galactose.
Bioorg Med Chem Lett 11: 459-62 (2001)
Novartis Pharma
First tricyclic oximino derivatives as 5-HT3 ligands.
Bioorg Med Chem Lett 11: 453-7 (2001)
Universit£
Synthesis and biological evaluation of novel amides of polyunsaturated fatty acids with dopamine.
Bioorg Med Chem Lett 11: 447-9 (2001)
Institute Of Bioorganic Chemistry Ras
5HT4(a) and 5-HT4(b) receptors have nearly identical pharmacology and are both expressed in human atrium and ventricle.
Naunyn Schmiedebergs Arch Pharmacol 363: 146-60 (2001)
University Of Oslo
Non-peptidic, non-prenylic inhibitors of the prenyl protein-specific protease Rce1.
Bioorg Med Chem Lett 11: 425-7 (2001)
Philipps-UniversitäT Marburg
Nipecotic and iso-nipecotic amides as potent and selective somatostatin subtype-2 receptor agonists.
Bioorg Med Chem Lett 11: 415-7 (2001)
Merck Research Laboratories
Synthesis and antifungal activities of novel 1,3-beta-D-glucan synthase inhibitors. Part 1.
Bioorg Med Chem Lett 11: 395-8 (2001)
Nippon Roche Research Center
Human beta3 adrenergic receptor agonists containing cyanoguanidine and nitroethylenediamine moieties.
Bioorg Med Chem Lett 11: 379-82 (2001)
Merck Research Laboratories
Synthesis and biological activity of novel potent endothelin-converting enzyme-1 inhibitors.
Bioorg Med Chem Lett 11: 375-8 (2001)
Novartis Institute For Biomedical Research
Serotonergic and dopaminergic activities of rigidified (R)-aporphine derivatives.
Bioorg Med Chem Lett 11: 367-70 (2001)
Uppsala University
Conformational study of a highly specific CXCR4 inhibitor, T140, disclosing the close proximity of its intrinsic pharmacophores associated with strong anti-HIV activity.
Bioorg Med Chem Lett 11: 359-62 (2001)
Kyoto University
The identification of alpha-ketoamides as potent inhibitors of hepatitis C virus NS3-4A proteinase.
Bioorg Med Chem Lett 11: 355-7 (2001)
Roche Discover Welwyn
The development of a potential single photon emission computed tomography (SPECT) imaging agent for the corticotropin-releasing hormone receptor type.
Bioorg Med Chem Lett 11: 331-3 (2001)
Niddk
Enkephalin analogues with 2',6'-dimethylphenylalanine replacing phenylalanine in position 4.
Bioorg Med Chem Lett 11: 327-9 (2001)
Tohoku Pharmaceutical University
Stereospecific synthesis of (2S)-2-methyl-3-(2',6'-dimethyl-4'-hydroxyphenyl)-propionic acid (Mdp) and its incorporation into an opioid peptide.
Bioorg Med Chem Lett 11: 323-5 (2001)
Clinical Research Institute Of Montreal
The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective alpha7 nicotinic receptor partial agonist.
Bioorg Med Chem Lett 11: 319-21 (2001)
Astrazeneca
Sulfonylated aminothiazoles as new small molecule inhibitors of protein phosphatases.
Bioorg Med Chem Lett 11: 313-7 (2001)
University Of Pittsburgh
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.
Bioorg Med Chem Lett 11: 309-12 (2001)
Dupont Pharmaceuticals
General synthesis of alpha-substituted 3-bisaryloxy propionic acid derivatives as specific MMP inhibitors.
Bioorg Med Chem Lett 11: 295-9 (2001)
Institut De Recherches Servier
Potent and selective bicyclic lactam inhibitors of thrombin. Part 4: transition state inhibitors.
Bioorg Med Chem Lett 11: 287-90 (2001)
Biochem Pharma
Synthesis and preliminary pharmacological evaluation of coumestans with different patterns of oxygenation.
Bioorg Med Chem Lett 11: 283-6 (2001)
Universidade Federal Do Rio De Janeiro
Synthesis of 7,8-disubstituted benzolactam-V8 and its binding to protein kinase C.
Bioorg Med Chem Lett 11: 99-101 (2001)
Institute Of Organic Chemistry
A disubstituted NAD+ analogue is a nanomolar inhibitor of trypanosomal glyceraldehyde-3-phosphate dehydrogenase.
Bioorg Med Chem Lett 11: 95-8 (2001)
University Of Washington
Arylalkylidene rhodanine with bulky and hydrophobic functional group as selective HCV NS3 protease inhibitor.
Bioorg Med Chem Lett 11: 91-4 (2001)
Institute Of Molecular And Cell Biology
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 2: structure-activity relationships for substituted 2-Aryl-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-(piperidin-1-yl)butanes.
Bioorg Med Chem Lett 11: 265-70 (2001)
Merck Research Laboratories
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. part 1: discovery and initial structure-activity relationships for 1 -amino-2-phenyl-4-(piperidin-1-yl)butanes.
Bioorg Med Chem Lett 11: 259-64 (2001)
Merck Research Laboratories
Polyamines with N-(3-phenylpropyl) substituents are effective competitive inhibitors of trypanothione reductase and trypanocidal agents.
Bioorg Med Chem Lett 11: 251-4 (2001)
Indiana State University
Intracellular inhibition of human neutrophil elastase by orally active pyrrolidine-trans-lactams.
Bioorg Med Chem Lett 11: 243-6 (2001)
Glaxowellcome Medicines Research Centre
Heteroaryl and cycloalkyl sulfonamide hydroxamic acid inhibitors of matrix metalloproteinases.
Bioorg Med Chem Lett 11: 239-42 (2001)
Wyeth-Ayerst Research
The discovery of anthranilic acid-based MMP inhibitors. Part 1: SAR of the 3-position.
Bioorg Med Chem Lett 11: 235-8 (2001)
Wyeth-Ayerst Research
Solid-phase optimisation of achiral amidinobenzyl indoles as potent and selective factor Xa inhibitors.
Bioorg Med Chem Lett 11: 227-30 (2001)
Aventis Pharma
Synthesis and dopaminergic properties of the two enantiomers of 3-(3,4-dimethylphenyl)-1-propylpiperidine, a potent and selective dopamine D4 receptor ligand.
Bioorg Med Chem Lett 11: 223-6 (2001)
Universit£
Design, synthesis, and biological evaluation of HIV/FIV protease inhibitors incorporating a conformationally constrained macrocycle with a small P3' residue.
Bioorg Med Chem Lett 11: 219-22 (2001)
The Scripps Research Institute
3,3a-Dihydropyrano[4,3,2-de]quinazolin-2(1H)-ones are potent non-nucleoside reverse transcriptase inhibitors.
Bioorg Med Chem Lett 11: 211-4 (2001)
Dupont Pharmaceuticals
Inhibition of hepatitis C virus NS3 protease activity by product-based peptides is dependent on helicase domain.
Bioorg Med Chem Lett 11: 203-6 (2001)
Uppsala University
Diastereoselective synthesis, activity and chiral stability of cyclic alkoxyketone inhibitors of cathepsin K.
Bioorg Med Chem Lett 11: 199-202 (2001)
Smithkline Beecham Pharmaceuticals
Solid-phase synthesis of cyclic alkoxyketones, inhibitors of the cysteine protease cathepsin K.
Bioorg Med Chem Lett 11: 195-8 (2001)
Smithkline Beecham Pharmaceuticals
High-pressure synthesis of enantiomerically pure C-6 substituted pyrazol.
Bioorg Med Chem Lett 11: 191-3 (2001)
Astrazeneca R&D Griffith University
3-Deoxy-3-substituted-D-myo-inositol imidazolyl ether lipid phosphates and carbonate as inhibitors of the phosphatidylinositol 3-kinase pathway and cancer cell growth.
Bioorg Med Chem Lett 11: 173-6 (2001)
Georgetown University Medical Center
2,2-Dimethyl-4,5-diaryl-3(2H)furanone derivatives as selective cyclo-oxygenase-2 inhibitors.
Bioorg Med Chem Lett 11: 165-8 (2001)
Pacific Corporation R & D Center
Synthesis and P2Y receptor activity of a series of uridine dinucleoside 5'-polyphosphates.
Bioorg Med Chem Lett 11: 157-60 (2001)
Inspire Pharmaceuticals
Design and synthesis of sialyl Lewis x mimics as E-selectin inhibitors.
Bioorg Med Chem Lett 11: 151-5 (2001)
Wyeth Research
Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 2.
Bioorg Med Chem Lett 11: 113-7 (2001)
Merck Research Laboratories
Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 1.
Bioorg Med Chem Lett 11: 107-11 (2001)
Merck Research Laboratories
Characterization of the antitumor effects of the selective farnesyl protein transferase inhibitor R115777 in vivo and in vitro.
Cancer Res 61: 131-7 (2001)
Janssen Research Foundation
Cloning of a chick A3 adenosine receptor: characterization of ligand binding and receptor-effector coupling of chick A1 and A3 adenosine receptors.
Naunyn Schmiedebergs Arch Pharmacol 363: 81-6 (2001)
University Of Illinois At Chicago
Apical uptake of organic cations by human intestinal Caco-2 cells: putative involvement of ASF transporters.
Naunyn Schmiedebergs Arch Pharmacol 363: 40-9 (2001)
Universidade Do Porto
Characterisation and comparison of novel ligands for the nociceptin/orphanin FQ receptor.
Naunyn Schmiedebergs Arch Pharmacol 363: 28-33 (2001)
Leicester Royal Infirmary
Energetic, structural, and antimicrobial analyses of beta-lactam side chain recognition by beta-lactamases.
Chem Biol 8: 17-31 (2001)
Northwestern University
Cloning, expression, and pharmacological characterization of a novel human histamine receptor.
Mol Pharmacol 59: 434-41 (2001)
Smithkline Beecham Pharmaceuticals
Discovery of a novel member of the histamine receptor family.
Mol Pharmacol 59: 427-33 (2001)
The Centre For Addiction And Mental Health
Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow.
Mol Pharmacol 59: 420-6 (2001)
The R. W. Johnson Pharmaceutical Research Institute
Antipsychotic drugs: importance of dopamine receptors for mechanisms of therapeutic actions and side effects.
Pharmacol Rev 53: 119-33 (2001)
University Of Reading
Two new stilbene dimer glucosides from grape (Vitis vinifera) cell cultures.
J Nat Prod 64: 136-8 (2001)
University Of Illinois At Chicago
Synthesis of a novel lysophosphatidylcholine.
J Nat Prod 64: 98-9 (2001)
Graduate School Of Okayama University
Isolation and structure determination of nostocyclopeptides A1 and A2 from the terrestrial cyanobacterium Nostoc sp. ATCC53789.
J Nat Prod 64: 54-9 (2001)
University Of Hawaii At Manoa
Structure-activity relationships at monoamine transporters and muscarinic receptors for N-substituted-3alpha-(3'-chloro-, 4'-chloro-, and 4',4''-dichloro-substituted-diphenyl)methoxytropanes.
J Med Chem 44: 633-40 (2001)
National Institute On Drug Abuse-Intramural Research Program
seco-Cyclothialidines: new concise synthesis, inhibitory activity toward bacterial and human DNA topoisomerases, and antibacterial properties.
J Med Chem 44: 619-26 (2001)
Bayer
AMP deaminase inhibitors. 5. Design, synthesis, and SAR of a highly potent inhibitor series.
J Med Chem 44: 613-8 (2001)
Metabasis Therapeutics
Novel glucocorticoid antedrugs possessing a 17beta-(gamma-lactone) ring.
J Med Chem 44: 602-12 (2001)
Glaxo Wellcome Research And Development
Discovery of 1-[3-(aminomethyl)phenyl]-N-3-fluoro-2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide (DPC423), a highly potent, selective, and orally bioavailable inhibitor of blood coagulation factor Xa.
J Med Chem 44: 566-78 (2001)
Dupont Pharmaceuticals
2- and 3-substituted 1,4-naphthoquinone derivatives as subversive substrates of trypanothione reductase and lipoamide dehydrogenase from Trypanosoma cruzi: synthesis and correlation between redox cycling activities and in vitro cytotoxicity.
J Med Chem 44: 548-65 (2001)
Umr 8525 Cnrs - Université
Coumarin and chromen-4-one analogues as tautomerase inhibitors of macrophage migration inhibitory factor: discovery and X-ray crystallography.
J Med Chem 44: 540-7 (2001)
Yamanouchi Pharmaceutical
Design, synthesis, and evaluation of novel A2A adenosine receptor agonists.
J Med Chem 44: 531-9 (2001)
University Of Virginia
Crystal structure of human cyclin-dependent kinase 2 in complex with the adenine-derived inhibitor H717.
J Med Chem 44: 524-30 (2001)
Lawrence Berkeley National Laboratory
Current and novel approaches to the drug treatment of schizophrenia.
J Med Chem 44: 477-501 (2001)
Merck Sharp And Dohme Research Laboratories
Nucleosides and nucleotides. 200. Reinvestigation of 5'-N-ethylcarboxamidoadenosine derivatives: structure-activity relationships for P(3) purinoceptor-like proteins.
J Med Chem 44: 208-14 (2001)
Hokkaido University
Synthesis and structure-activity relationships of a new model of arylpiperazines. Study of the 5-HT(1a)/alpha(1)-adrenergic receptor affinity by classical hansch analysis, artificial neural networks, and computational simulation of ligand recognition.
J Med Chem 44: 198-207 (2001)
Universidad Complutense
Synthesis and structure-activity relationships of a new model of arylpiperazines. 5. Study of the physicochemical influence of the pharmacophore on 5-HT(1a)/alpha(1)-adrenergic receptor affinity: synthesis of a new derivative with mixed 5-HT(1a)/d(2) antagonist properties.
J Med Chem 44: 186-97 (2001)
Universidad Complutense
2-Alkynyl-8-aryl-9-methyladenines as novel adenosine receptor antagonists: their synthesis and structure-activity relationships toward hepatic glucose production induced via agonism of the A(2B) receptor.
J Med Chem 44: 170-9 (2001)
Eisai
Synthesis and comparative molecular field analysis (CoMFA) of symmetric and nonsymmetric cyclic sulfamide HIV-1 protease inhibitors.
J Med Chem 44: 155-69 (2001)
Uppsala University
Estimation of binding affinities for HEPT and nevirapine analogues with HIV-1 reverse transcriptase via Monte Carlo simulations.
J Med Chem 44: 145-54 (2001)
Yale University
Stereochemistry and molecular pharmacology of (S)-thio-ATPA, a new potent and selective GluR5 agonist.
Eur J Pharmacol 411: 245-53 (2001)
The Royal Danish School Of Pharmacy
Pharmacological properties of the potent epileptogenic amino acid dysiherbaine, a novel glutamate receptor agonist isolated from the marine sponge Dysidea herbacea.
J Pharmacol Exp Ther 296: 650-8 (2001)
Kitasato University
Etoricoxib (MK-0663): preclinical profile and comparison with other agents that selectively inhibit cyclooxygenase-2.
J Pharmacol Exp Ther 296: 558-66 (2001)
Merck Frosst Centre For Therapeutic Research
In vitro and in vivo pharmacological characterization of JTE-907, a novel selective ligand for cannabinoid CB2 receptor.
J Pharmacol Exp Ther 296: 420-5 (2001)
Japan Tobacco
Extended TIP(P) analogues as precursors for labeled delta-opioid receptor ligands.
J Med Chem 43: 5050-4 (2001)
University Of Maryland
Synthesis and evaluation of isothiocyanate-containing derivatives of the delta-opioid receptor antagonist Tyr-Tic-Phe-Phe (TIPP) as potential affinity labels for delta-opioid receptors.
J Med Chem 43: 5044-9 (2001)
University Of Maryland
Optimization of substituted N-3-benzylimidazoquinazolinone sulfonamides as potent and selective PDE5 inhibitors.
J Med Chem 43: 5037-43 (2001)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and in vitro and in vivo activity of (-)-(1R,5R,9R)- and (+)-(1S,5S,9S)-N-alkenyl-, -N-alkynyl-, and -N-cyanoalkyl-5, 9-dimethyl-2'-hydroxy-6,7-benzomorphan homologues.
J Med Chem 43: 5030-6 (2001)
Virginia Commonwealth University
A potent, long-acting, orally active (2R)-2-[(1R)-3, 3-difluorocyclopentyl]-2-hydroxy-2-phenylacetamide: novel muscarinic M(3) receptor antagonist with high selectivity for M(3) over M(2) receptors.
J Med Chem 43: 5017-29 (2001)
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist.
J Med Chem 43: 5010-6 (2001)
Schering
5-Azidoimidacloprid and an acyclic analogue as candidate photoaffinity probes for mammalian and insect nicotinic acetylcholine receptors.
J Med Chem 43: 5003-9 (2001)
University Of California
D-Amino acid scan of gamma-melanocyte-stimulating hormone: importance of Trp(8) on human MC3 receptor selectivity.
J Med Chem 43: 4998-5002 (2001)
University Of Arizona
Slow-onset, long-duration 3-(3',4'-dichlorophenyl)-1-indanamine monoamine reuptake blockers as potential medications to treat cocaine abuse.
J Med Chem 43: 4981-92 (2001)
Pharm-Eco Laboratories
Fluorosulfonyl-substituted xanthines as selective irreversible antagonists for the A(1)-adenosine receptor.
J Med Chem 43: 4973-80 (2001)
Deakin University
A novel series of 4-piperidinopyridine and 4-piperidinopyrimidine inhibitors of 2,3-oxidosqualene cyclase-lanosterol synthase.
J Med Chem 43: 4964-72 (2001)
Astrazeneca
Development of new hydroxamate matrix metalloproteinase inhibitors derived from functionalized 4-aminoprolines.
J Med Chem 43: 4948-63 (2001)
Procter And Gamble Pharmaceuticals
Design and synthesis of new orally active nonpeptidic inhibitors of human neutrophil elastase.
J Med Chem 43: 4927-9 (2001)
Colorado State University
4-Aryl-2,4-dioxobutanoic acid inhibitors of HIV-1 integrase and viral replication in cells.
J Med Chem 43: 4923-6 (2001)
Merck Research Laboratories
Chalcone derivatives antagonize interactions between the human oncoprotein MDM2 and p53.
Biochemistry 40: 336-44 (2001)
Max Planck Institute
Inhibitory potencies of 1,4-dihydropyridine calcium antagonists to P-glycoprotein-mediated transport: comparison with the effects on CYP3A4.
Pharm Res 17: 1189-97 (2000)
Kanazawa University
Three new arylobenzofurans from Onobrychis ebenoides and evaluation of their binding affinity for the estrogen receptor.
J Nat Prod 63: 1672-4 (2001)
University Of Athens
Guaiane dimers and germacranolide from Artemisia caruifolia.
J Nat Prod 63: 1626-9 (2000)
Toyama Medical And Pharmaceutical University
Hexahydrochromeno[4,3-b]pyrrole derivatives as acetylcholinesterase inhibitors.
J Med Chem 44: 105-9 (2001)
University Of Bologna
Novel, nonpeptidic cyanamides as potent and reversible inhibitors of human cathepsins K and L.
J Med Chem 44: 94-104 (2001)
Merck Frosst Centre For Therapeutic Research
Terminally alkylated polyamine analogues as chemotherapeutic agents.
J Med Chem 44: 1-26 (2001)
Wayne State University
p38 kinase inhibitors for the treatment of arthritis and osteoporosis: thienyl, furyl, and pyrrolyl ureas.
Bioorg Med Chem Lett 11: 9-12 (2001)
Bayer Research Center
Structure-activity studies of 5-substituted pyridopyrimidines as adenosine kinase inhibitors.
Bioorg Med Chem Lett 11: 83-6 (2001)
Abbott Laboratories
B-ring substituted 5,7-dihydroxyflavonols with high-affinity binding to P-glycoprotein responsible for cell multidrug resistance.
Bioorg Med Chem Lett 11: 75-7 (2001)
DéPartement De Pharmacochimie MoléCulaire Umr-Cnrs 5063
Inhibition of RANTES/CCR1-mediated chemotaxis by cosalane and related compounds.
Bioorg Med Chem Lett 11: 59-62 (2001)
National Cancer Istitute-Frederick Cancer Research And Development Center
Phenyl benzenesulfonamides are novel and selective 5-HT6 antagonists: identification of N-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide (SB-357134).
Bioorg Med Chem Lett 11: 55-8 (2001)
Smithkline Beecham Pharmaceuticals
Antimitotic and cell growth inhibitory properties of combretastatin A-4-like ethers.
Bioorg Med Chem Lett 11: 51-4 (2001)
The University Of Manchester
Phthalazine PDE4 inhibitors. Part 2: the synthesis and biological evaluation of 6-methoxy-1,4-disubstituted derivatives.
Bioorg Med Chem Lett 11: 33-7 (2001)
Zambon Group
Allosteric inhibition of fructose-1,6-bisphosphatase by anilinoquinazolines.
Bioorg Med Chem Lett 11: 17-21 (2001)
Pfizer
Imide and lactam derivatives of N-benzylpyroglutamyl-L-phenylalanine as VCAM/VLA-4 antagonists.
Bioorg Med Chem Lett 11: 1-4 (2001)
Hoffmann-La Roche
Synthesis and structure-activity relationships of 3-cyano-4-(phenoxyanilino)quinolines as MEK (MAPKK) inhibitors.
Bioorg Med Chem Lett 10: 2825-8 (2000)
Wyeth-Ayerst Research
Synthesis and activity of selective MMP inhibitors with an aryl backbone.
Bioorg Med Chem Lett 10: 2815-7 (2000)
Pharmacia
A novel pyridazinone derivative as a nonprostanoid PGI2 agonist.
Bioorg Med Chem Lett 10: 2787-90 (2000)
Fujisawa Pharmaceutical
Evaluation of new L-thiocitrulline derivatives as inhibitors of nitric oxide synthase.
Bioorg Med Chem Lett 10: 2779-81 (2000)
Wake Forest University
Noncovalent thrombin inhibitors incorporating an imidazolylethynyl P1.
Bioorg Med Chem Lett 10: 2775-8 (2000)
Lg Chemical
1H-pyrazole-1-carboxamidines: new inhibitors of nitric oxide synthase.
Bioorg Med Chem Lett 10: 2771-4 (2000)
Northwestern University
Synthesis and binding activity of endomorphin-1 analogues containing beta-amino acids.
Bioorg Med Chem Lett 10: 2755-8 (2000)
Universit£
Assessment of substitution in the second pharmacophore of Dmt-Tic analogues.
Bioorg Med Chem Lett 10: 2745-8 (2000)
University Of Naples
A convenient procedure for the synthesis of nonsymmetrical bivalent selective serotonin reuptake inhibitors using polymer-supported reagents.
Bioorg Med Chem Lett 10: 2741-3 (2000)
Georgetown University Medical Center
Optimization of a somatostatin mimetic via constrained amino acid and backbone incorporation.
Bioorg Med Chem Lett 10: 2731-3 (2000)
University Of California
Benzylidene ketal derivatives as M2 muscarinic receptor antagonists.
Bioorg Med Chem Lett 10: 2727-30 (2000)
Schering-Plough Research Institute
Determination of the relative and absolute stereochemistry of a potent and alpha1A-selective adrenoceptor antagonist.
Bioorg Med Chem Lett 10: 2705-7 (2000)
Synaptic Pharmaceutical
3-(4-Piperidinyl)- and 3-(8-aza-bicyclo[3.2.1]oct-3-yl)-2-phenyl-1H-indoles as bioavailable h5-HT2A antagonists.
Bioorg Med Chem Lett 10: 2701-3 (2000)
Merck Sharp & Dohme Research Laboratories
2-Aryl tryptamines: selective high-affinity antagonists for the h5-HT2A receptor.
Bioorg Med Chem Lett 10: 2697-9 (2000)
Merck Sharp & Dohme Research Laboratories
Solid-phase synthesis of 2,3-disubstituted indoles: discovery of a novel, high-affinity, selective h5-HT2A antagonist.
Bioorg Med Chem Lett 10: 2693-6 (2000)
Merck Sharp & Dohme Research Laboratories
Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds.
Life Sci 68: 29-39 (2000)
Mayo Foundation
Synthesis, characterization, and activity of metabolites derived from the cyclooxygenase-2 inhibitor rofecoxib (MK-0966, Vioxx).
Bioorg Med Chem Lett 10: 2683-6 (2000)
Merck Frosst Centre For Therapeutic Research
Synthesis and biological evaluation of 2,5-dihydropyrazol.
Bioorg Med Chem Lett 10: 2661-4 (2000)
RhôNe-Poulenc Rorer
Synthesis and characterization of a potent and selective protein tyrosine phosphatase inhibitor, 2.
Bioorg Med Chem Lett 10: 2657-60 (2000)
Taisho Pharmaceutical
(S)-Thiirancarboxylic acid as a reactive building block for a new class of cysteine protease inhibitors.
Bioorg Med Chem Lett 10: 2647-51 (2000)
University Of WüRzburg
Serotonin transporter inhibitors: synthesis and binding potency of 2'-methyl- and 3'-methyl-6-nitroquipazine.
Bioorg Med Chem Lett 10: 2643-6 (2000)
Central Washington University
Pharmacophore identification of a specific CXCR4 inhibitor, T140, leads to development of effective anti-HIV agents with very high selectivity indexes.
Bioorg Med Chem Lett 10: 2633-7 (2000)
Kyoto University
6-Hydroxy-1,3-dioxin-4-ones as non-peptidic HIV protease inhibitors.
Bioorg Med Chem Lett 10: 2625-7 (2000)
Institute Of Science & Technology
Synthesis of apicidin-derived quinolone derivatives: parasite-selective histone deacetylase inhibitors and antiproliferative agents.
J Med Chem 43: 4919-22 (2000)
Merck Research Laboratories
Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
J Med Chem 43: 4893-909 (2000)
Taisho Pharmaceutical
Carbonic anhydrase inhibitors: water-soluble 4-sulfamoylphenylthioureas as topical intraocular pressure-lowering agents with long-lasting effects.
J Med Chem 43: 4884-92 (2000)
Universit£
Design, synthesis, and monoamine transporter binding site affinities of methoxy derivatives of indatraline.
J Med Chem 43: 4868-76 (2000)
National Institute Of Diabetes And Digestive And Kidney Diseases
Synthesis, structure-activity relationships, and pharmacological profile of 9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6, 7,1-hi]indoles: discovery of potent, selective phosphodiesterase type 4 inhibitors.
J Med Chem 43: 4850-67 (2000)
Pfizer
Synthesis and transporter binding properties of bridged piperazine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909).
J Med Chem 43: 4840-9 (2000)
National Institute Of Diabetes And Digestive And Kidney Diseases
Semisynthesis of antitumoral acetogenins: SAR of functionalized alkyl-chain bis-tetrahydrofuranic acetogenins, specific inhibitors of mitochondrial complex I.
J Med Chem 43: 4793-800 (2000)
Universidad De Valencia
Design of adenosine kinase inhibitors from the NMR-based screening of fragments.
J Med Chem 43: 4781-6 (2000)
Abbott Laboratories
Pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists: influence of the chain at the N(8) pyrazole nitrogen.
J Med Chem 43: 4768-80 (2000)
Università
Inhibition of monoamine oxidases by functionalized coumarin derivatives: biological activities, QSARs, and 3D-QSARs.
J Med Chem 43: 4747-58 (2000)
Universit£
Synthesis and in vitro opioid activity profiles of DALDA analogues.
Eur J Med Chem 35: 895-901 (2000)
Clinical Research Institute Of Montreal
Pharmacological profiles of the metabotropic glutamate receptor ligands.
Neuropharmacology 40: 170-7 (2001)
University Of Toronto
Estimation of the hydrophobic effect in an antigen-antibody protein-protein interface.
Biochemistry 39: 15375-87 (2000)
University Of Maryland Biotechnology Institute
Agonists and antagonists acting at P2X receptors: selectivity profiles and functional implications.
Naunyn Schmiedebergs Arch Pharmacol 362: 340-50 (2000)
Biocentre Niederursel
Evidence for possible involvement of 5-HT(2B) receptors in the cardiac valvulopathy associated with fenfluramine and other serotonergic medications.
Circulation 102: 2836-41 (2000)
Nih
Glutathione stimulates sulfated estrogen transport by multidrug resistance protein 1.
J Biol Chem 276: 6404-11 (2001)
Queen'S University
Characterisation of human monocarboxylate transporter 4 substantiates its role in lactic acid efflux from skeletal muscle.
J Physiol (Lond) 529: 285-93 (2000)
University Of Bristol
Effect of ring fluorination on the pharmacology of hallucinogenic tryptamines.
J Med Chem 43: 4701-10 (2001)
Purdue University
Adenosine deaminase inhibitors: synthesis and biological evaluation of unsaturated, aromatic, and oxo derivatives of (+)-erythro-9-(2'S-hydroxy-3'R-nonyl)adenine [(+)-EHNA].
J Med Chem 43: 4694-700 (2001)
University Of Rhode Island
4-Aminoquinolines: novel nociceptin antagonists with analgesic activity.
J Med Chem 43: 4667-77 (2001)
Central Pharmaceutical Research Institute
New tacrine-huperzine A hybrids (huprines): highly potent tight-binding acetylcholinesterase inhibitors of interest for the treatment of Alzheimer's disease.
J Med Chem 43: 4657-66 (2001)
Universitat De Barcelona
5-Substituted N(4)-hydroxy-2'-deoxycytidines and their 5'-monophosphates: synthesis, conformation, interaction with tumor thymidylate synthase, and in vitro antitumor activity.
J Med Chem 43: 4647-56 (2001)
Polish Academy Of Sciences
7-Deazaadenines bearing polar substituents: structure-activity relationships of new A(1) and A(3) adenosine receptor antagonists.
J Med Chem 43: 4636-46 (2001)
University Of Leipzig
Chiral derivatives of 2-cyclohexylideneperhydro-4,7-methanoindenes, a novel class of nonsteroidal androgen receptor ligand: synthesis, X-ray analysis, and biological activity.
J Med Chem 43: 4629-35 (2001)
The University Of Sydney
Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases.
J Med Chem 43: 4606-16 (2000)
Parke-Davis Pharmaceutical Research
1,3-Diaryl-4,5,6,7-tetrahydro-2H-isoindole derivatives: a new series of potent and selective COX-2 inhibitors in which a sulfonyl group is not a structural requisite.
J Med Chem 43: 4582-93 (2001)
Institut De Recherche Servier
Discovery of chiral N,N-disubstituted trifluoro-3-amino-2-propanols as potent inhibitors of cholesteryl ester transfer protein.
J Med Chem 43: 4575-8 (2001)
Pfizer
Interaction between methotrexate and nonsteroidal anti-inflammatory drugs in organic anion transporter.
Eur J Pharmacol 409: 31-6 (2001)
Kyoto University Hospital
SST3-selective potent peptidic somatostatin receptor antagonists.
Proc Natl Acad Sci U S A 97: 13973-8 (2000)
University Of Berne
Molecular cloning and characterization of a second human cysteinyl leukotriene receptor: discovery of a subtype selective agonist.
Mol Pharmacol 58: 1601-8 (2000)
University Of California Irvine
Synthetic modification of prostaglandin f(2alpha) indicates different structural determinants for binding to the prostaglandin F receptor versus the prostaglandin transporter.
Mol Pharmacol 58: 1511-6 (2000)
Albert Einstein College Of Medicine
Correlation of the apparent affinities and efficacies of gamma-aminobutyric acid(C) receptor agonists.
Mol Pharmacol 58: 1375-80 (2000)
University Of Alabama At Birmingham
Characterization of the binding site for a novel class of noncompetitive alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor antagonists.
Mol Pharmacol 58: 1310-7 (2000)
Pfizer
Structural determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin, and staurosporine.
Mol Cell 6: 909-19 (2000)
Mrc
Cyanoindole derivatives as highly selective dopamine D(4) receptor partial agonists: solid-phase synthesis, binding assays, and functional experiments.
J Med Chem 43: 4563-9 (2000)
Friedrich-Alexander University
Synthesis, (18)F-labeling, and biological evaluation of piperidyl and pyrrolidyl benzilates as in vivo ligands for muscarinic acetylcholine receptors.
J Med Chem 43: 4552-62 (2000)
University Of Michigan Medical School
Carbonic anhydrase inhibitors: perfluoroalkyl/aryl-substituted derivatives of aromatic/heterocyclic sulfonamides as topical intraocular pressure-lowering agents with prolonged duration of action.
J Med Chem 43: 4542-51 (2000)
Universit£
Solid-phase synthesis and biological evaluation of a combinatorial library of philanthotoxin analogues.
J Med Chem 43: 4526-33 (2000)
The Royal Danish School Of Pharmacy
Syntheses of 4'-C-ethynyl-beta-D-arabino- and 4'-C-ethynyl-2'-deoxy-beta-D-ribo-pentofuranosylpyrimidines and -purines and evaluation of their anti-HIV activity.
J Med Chem 43: 4516-25 (2000)
Tohoku University
6-Alkylamino- and 2,3-dihydro-3'-methoxy-2-phenyl-4-quinazolinones and related compounds: their synthesis, cytotoxicity, and inhibition of tubulin polymerization.
J Med Chem 43: 4479-87 (2000)
China Medical College
Structure-activity relationships of 17alpha-derivatives of estradiol as inhibitors of steroid sulfatase.
J Med Chem 43: 4465-78 (2000)
Laval University
Design and synthesis of pyrrolidine-5,5-trans-lactams (5-oxo-hexahydro-pyrrolo[3,2-b]pyrroles) as novel mechanism-based inhibitors of human cytomegalovirus protease. 1. The alpha-methyl-trans-lactam template.
J Med Chem 43: 4452-64 (2000)
Glaxo Wellcome Research And Development
Computational studies on HIV-1 protease inhibitors: influence of calculated inhibitor-enzyme binding affinities on the statistical quality of 3D-QSAR CoMFA models.
J Med Chem 43: 4446-51 (2000)
University Of Missouri St. Louis
Synthesis and evaluation of 17-aliphatic heterocycle-substituted steroidal inhibitors of 17alpha-hydroxylase/C17-20-lyase (P450 17).
J Med Chem 43: 4437-45 (2000)
University Of The Saarland
Chiral resolution, pharmacological characterization, and receptor docking of the noncompetitive mGlu1 receptor antagonist (+/-)-2-hydroxyimino- 1a, 2-dihydro-1H-7-oxacyclopropa[b]naphthalene-7a-carboxylic acid ethyl ester.
J Med Chem 43: 4428-36 (2000)
Novartis Pharma
Multiple-conformation and protonation-state representation in 4D-QSAR: the neurokinin-1 receptor system.
J Med Chem 43: 4416-27 (2000)
Biographics Laboratory 3R
Design, synthesis, and biological evaluation of potent and selective amidino bicyclic factor Xa inhibitors.
J Med Chem 43: 4398-415 (2000)
Dupont Pharmaceuticals
Novel design of nonpeptide AVP V(2) receptor agonists: structural requirements for an agonist having 1-(4-aminobenzoyl)-2,3,4, 5-tetrahydro-1H-1-benzazepine as a template.
J Med Chem 43: 4388-97 (2000)
Otsuka Pharmaceutical
Structure-function studies on the new growth hormone-releasing peptide, ghrelin: minimal sequence of ghrelin necessary for activation of growth hormone secretagogue receptor 1a.
J Med Chem 43: 4370-6 (2000)
Merck Research Laboratories
Design, radiosynthesis, and biodistribution of a new potent and selective ligand for in vivo imaging of the adenosine A(2A) receptor system using positron emission tomography.
J Med Chem 43: 4359-62 (2000)
University Of Milano-Bicocca
Biarylpropylsulfonamides as novel, potent potentiators of 2-amino-3- (5-methyl-3-hydroxyisoxazol-4-yl)- propanoic acid (AMPA) receptors.
J Med Chem 43: 4354-8 (2000)
Nps Allelix
Potent nonpeptide endothelin antagonists: synthesis and structure-activity relationships of pyrazole-5-carboxylic acids.
Bioorg Med Chem Lett 10: 2575-8 (2001)
Hoechst Marion Roussel
Synthesis of the novel analogues of dysidiolide and their structure-activity relationship.
Bioorg Med Chem Lett 10: 2571-4 (2001)
The University Of Tokyo
Arylacetamides as peripherally restricted kappa opioid receptor agonists.
Bioorg Med Chem Lett 10: 2567-70 (2001)
Adolor
N-1 substituted pyrimidin-4-ones: novel, orally active inhibitors of lipoprotein-associated phospholipase A2.
Bioorg Med Chem Lett 10: 2557-61 (2001)
Smithkline Beecham Pharmaceuticals
Novel 2,3,4,5-tetrahydro-1H-3-benzazepines with high affinity and selectivity for the dopamine D3 receptor.
Bioorg Med Chem Lett 10: 2553-5 (2000)
Smithkline Beecham Pharmaceuticals
Androsterone 3beta-substituted derivatives as inhibitors of type 3 17beta-hydroxysteroid dehydrogenase.
Bioorg Med Chem Lett 10: 2533-6 (2001)
Laval University
Bisquaternary caracurine V derivatives as allosteric modulators of ligand binding to M2 acetylcholine receptors.
Bioorg Med Chem Lett 10: 2529-32 (2001)
University Of WüRzburg
Inhibition of vertebrate squalene epoxidase by isoprenyl gallates and phenylalkyl gallates.
Bioorg Med Chem Lett 10: 2525-8 (2001)
University Of Shizuoka
Solid-phase synthesis of di- and tripeptidic hydroxamic acids as inhibitors of procollagen C-proteinase.
Bioorg Med Chem Lett 10: 2513-6 (2001)
Roche Bioscience
Synthesis and calpain inhibitory activity of alpha-ketoamides with 2,3-methanoleucine stereoisomers at the P2 position.
Bioorg Med Chem Lett 10: 2497-500 (2001)
The University Of Tennessee Health Science Center
S18616, a highly potent, spiroimidazoline agonist at alpha(2)-adrenoceptors: I. Receptor profile, antinociceptive and hypothermic actions in comparison with dexmedetomidine and clonidine.
J Pharmacol Exp Ther 295: 1192-205 (2000)
Centre De Recherches De Croissy
ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse.
J Pharmacol Exp Ther 295: 1156-64 (2000)
Abbott Laboratories
Characterization of [(3)H]Quisqualate binding to recombinant rat metabotropic glutamate 1a and 5a receptors and to rat and human brain sections.
J Neurochem 75: 2590-601 (2000)
F. Hoffmann-La Roche
Inhibitors of src tyrosine kinase: the preparation and structure-activity relationship of 4-anilino-3-cyanoquinolines and 4-anilinoquinazolines.
Bioorg Med Chem Lett 10: 2477-80 (2000)
Wyeth-Ayerst Research
Synthesis, chiral chromatographic separation, and biological activities of the enantiomers of 10,10-dimethylhuperzine A.
Bioorg Med Chem Lett 10: 2467-9 (2001)
Georgetown University Medical Center
N-[1-(2-Phenylethyl)pyrrolidin-3-yl]-1-adamantanecarboxamides as novel 5-HT2 receptor antagonists.
Bioorg Med Chem Lett 10: 2457-61 (2001)
Welfide
N-Cyclohexylethyl-N-noroxymorphindole: a mu-opioid preferring analogue of naltrindole.
Bioorg Med Chem Lett 10: 2449-51 (2001)
University Of Maryland
3alpha-(4-Substituted phenyl)nortropane-2beta-carboxylic acid methyl esters show selective binding at the norepinephrine transporter.
Bioorg Med Chem Lett 10: 2445-7 (2001)
Research Triangle Institute
Synthesis of glutaminyl adenylate analogues that are inhibitors of glutaminyl-tRNA synthetase.
Bioorg Med Chem Lett 10: 2441-4 (2001)
Universit£
Multistep solution-phase parallel synthesis of spiperone analogues.
Bioorg Med Chem Lett 10: 2435-9 (2001)
Acadia Pharmaceuticals
Structure-based design of six novel classes of nonpeptide antagonists of the bradykinin B2 receptor.
Bioorg Med Chem Lett 10: 2421-5 (2001)
Roche Bioscience
Syntheses of optically pure beta-hydroxyaspartate derivatives as glutamate transporter blockers.
Bioorg Med Chem Lett 10: 2407-10 (2001)
Institute For Bioorganic Research
1-Oxacephem-based human chymase inhibitors: discovery of stable inhibitors in human plasma.
Bioorg Med Chem Lett 10: 2403-6 (2001)
Shionogi
Synthesis and structure-activity relationships of a new class of 1-oxacephem-based human chymase inhibitors.
Bioorg Med Chem Lett 10: 2397-401 (2001)
Shionogi
A new 7,8-euphadien-type triterpenoid from Brackenridgea nitida and Bleasdalea bleasdalei that inhibits DNA polymerase beta.
J Nat Prod 63: 1356-60 (2000)
University Of Virginia
Amphetamine-type central nervous system stimulants release norepinephrine more potently than they release dopamine and serotonin.
Synapse 39: 32-41 (2001)
Nih
Structure-activity relationships of a series of pyrrolo[3,2-d]pyrimidine derivatives and related compounds as neuropeptide Y5 receptor antagonists.
J Med Chem 43: 4288-312 (2000)
Amgen
Synthesis and evaluation of novel steroidal oxime inhibitors of P450 17 (17 alpha-hydroxylase/C17-20-lyase) and 5 alpha-reductase types 1 and 2.
J Med Chem 43: 4266-77 (2000)
University Of The Saarland
3-(3,5-Dimethoxyphenyl)-1,6-naphthyridine-2,7-diamines and related 2-urea derivatives are potent and selective inhibitors of the FGF receptor-1 tyrosine kinase.
J Med Chem 43: 4200-11 (2000)
University Of Auckland
The mitochondrial monoamine oxidase-aldehyde dehydrogenase pathway: a potential site of action of daidzin.
J Med Chem 43: 4169-79 (2000)
Harvard Medical School
2D QSAR modeling and preliminary database searching for dopamine transporter inhibitors using genetic algorithm variable selection of Molconn Z descriptors.
J Med Chem 43: 4151-9 (2000)
National Institute On Drug Abuse-Intramural Research Program
Adenosine analogues as inhibitors of Trypanosoma brucei phosphoglycerate kinase: elucidation of a novel binding mode for a 2-amino-N(6)-substituted adenosine.
J Med Chem 43: 4135-50 (2000)
University Of Washington
Thio- and oxoflavopiridols, cyclin-dependent kinase 1-selective inhibitors: synthesis and biological effects.
J Med Chem 43: 4126-34 (2000)
Bristol-Myers Squibb Pharmaceutical Research Institute
Active site binding modes of HIV-1 integrase inhibitors.
J Med Chem 43: 4109-17 (2000)
University Of California
3D-QSAR CoMFA on cyclin-dependent kinase inhibitors.
J Med Chem 43: 4098-108 (2000)
Institut Curie
Resistance-modifying agents. 9. Synthesis and biological properties of benzimidazole inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase.
J Med Chem 43: 4084-97 (2000)
Newcastle University
Resistance-modifying agents. 8. Inhibition of O(6)-alkylguanine-DNA alkyltransferase by O(6)-alkenyl-, O(6)-cycloalkenyl-, and O(6)-(2-oxoalkyl)guanines and potentiation of temozolomide cytotoxicity in vitro by O(6)-(1-cyclopentenylmethyl)guanine.
J Med Chem 43: 4071-83 (2000)
Newcastle University
Rational design, synthesis, and biological activity of benzoxazinones as novel factor Xa inhibitors.
J Med Chem 43: 4063-70 (2000)
Pfizer
Synthesis of phenalene and acenaphthene derivatives as new conformationally restricted ligands for melatonin receptors.
J Med Chem 43: 4051-62 (2000)
Paris-Sud University
(-)-Spiro[1-azabicyclo[2.2.2]octane-3,5'-oxazolidin-2'-one], a conformationally restricted analogue of acetylcholine, is a highly selective full agonist at the alpha 7 nicotinic acetylcholine receptor.
J Med Chem 43: 4045-50 (2000)
Astrazeneca R&D Boston
Discovery of potent cyclic pseudopeptide human tachykinin NK-2 receptor antagonists.
J Med Chem 43: 4041-4 (2000)
Menarini Ricerche
Synthesis and estrogen receptor binding affinities of novel pyrrolo[2,1,5-cd]indolizine derivatives.
Bioorg Med Chem Lett 10: 2383-6 (2000)
Novo Nordisk
Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H3-receptor antagonists.
Bioorg Med Chem Lett 10: 2379-82 (2001)
Freie UniversitäT Berlin
Novel heterocycles as selective alpha1-adrenergic receptor antagonists.
Bioorg Med Chem Lett 10: 2375-7 (2001)
The R. W. Johnson Pharmaceutical Research Institute
Optimising inhibitors of trypanothione reductase using solid-phase chemistry.
Bioorg Med Chem Lett 10: 2367-9 (2001)
University Of Southamton
Dibasic inhibitors of human mast cell tryptase. Part 2: structure-activity relationships and requirements for potent activity.
Bioorg Med Chem Lett 10: 2361-6 (2001)
Axys Pharmaceuticals
Dibasic inhibitors of human mast cell tryptase. Part 1: synthesis and optimization of a novel class of inhibitors.
Bioorg Med Chem Lett 10: 2357-60 (2001)
Axys Pharmaceuticals
Structure-based design and synthesis of phosphinate isosteres of phosphotyrosine for incorporation in Grb2-SH2 domain inhibitors. Part 1.
Bioorg Med Chem Lett 10: 2337-41 (2001)
Novartis Pharmaceuticals
Synthesis and NK1/NK2 receptor activity of substituted-4(Z)-(methoxyimino)pentyl-1-piperazines.
Bioorg Med Chem Lett 10: 2333-5 (2001)
Schering-Plough Research Institute
The design and synthesis of novel NK1/NK2 dual antagonists.
Bioorg Med Chem Lett 10: 2329-32 (2001)
Schering-Plough Research Institute
Novel, potent and selective chimeric FXa inhibitors featuring hydrophobic P1-ketoamide moieties.
Bioorg Med Chem Lett 10: 2305-9 (2001)
Corvas International
N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists.
Bioorg Med Chem Lett 10: 2295-9 (2001)
Virginia Commonwealth University
Tetrahydroisoquinoline derivatives containing a benzenesulfonamide moiety as potent, selective human beta3 adrenergic receptor agonists.
Bioorg Med Chem Lett 10: 2283-6 (2001)
Merck Research Laboratories
Metal mediated protease inhibition: design and synthesis of inhibitors of the human cytomegalovirus (hCMV) protease.
Bioorg Med Chem Lett 10: 2279-82 (2001)
Smithkline Beecham Pharmaceuticals
NMR line-broadening and transferred NOESY as a medicinal chemistry tool for studying inhibitors of the hepatitis C virus NS3 protease domain.
Bioorg Med Chem Lett 10: 2271-4 (2001)
Boehringer Ingelheim Pharmaceuticals
Highly potent and selective peptide-based inhibitors of the hepatitis C virus serine protease: towards smaller inhibitors.
Bioorg Med Chem Lett 10: 2267-70 (2001)
Boehringer Ingelheim Pharmaceuticals
Analogues of SB-203207 as inhibitors of tRNA synthetases.
Bioorg Med Chem Lett 10: 2263-6 (2001)
Australian National University
Selective kappa-opioid antagonists related to naltrindole. Effect of side-chain spacer in the 5'-amidinoalkyl series.
Bioorg Med Chem Lett 10: 2259-61 (2001)
University Of Bristol
Diphenyl sulfoxides as selective antagonists of the muscarinic M2 receptor.
Bioorg Med Chem Lett 10: 2255-7 (2001)
Schering-Plough Research Institute
Differential antibacterial activity of moenomycin analogues on gram-positive bacteria.
Bioorg Med Chem Lett 10: 2251-4 (2000)
Advanced Medicine
Design and synthesis of piperidinyl piperidine analogues as potent and selective M2 muscarinic receptor antagonists.
Bioorg Med Chem Lett 10: 2247-50 (2001)
Schering-Plough Research Institute
Discovery of novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intracellular adhesion molecule-1 interaction. 1. Identification of an additional binding pocket based on an anilino diaryl sulfide lead.
J Med Chem 43: 4025-40 (2000)
Abbott Laboratories
Inhibitors of NF-kappaB and AP-1 gene expression: SAR studies on the pyrimidine portion of 2-chloro-4-trifluoromethylpyrimidine-5-[N-(3', 5'-bis(trifluoromethyl)phenyl)carboxamide].
J Med Chem 43: 3995-4004 (2000)
Signal Pharmaceuticals
Novel histamine H(3)-receptor antagonists with carbonyl-substituted 4-(3-(phenoxy)propyl)-1H-imidazole structures like ciproxifan and related compounds.
J Med Chem 43: 3987-94 (2000)
Freie Universit£T Berlin
Role of hydrophobic interactions in binding S-(N-aryl/alkyl-N-hydroxycarbamoyl)glutathiones to the active site of the antitumor target enzyme glyoxalase I.
J Med Chem 43: 3981-6 (2000)
University Of Maryland
Synthesis and antiviral activity of 4-benzyl pyridinone derivatives as potent and selective non-nucleoside human immunodeficiency virus type 1 reverse transcriptase inhibitors.
J Med Chem 43: 3949-62 (2000)
Institut Curie
Synthesis and evaluation of N,N-dialkyl enkephalin-based affinity labels for delta opioid receptors.
J Med Chem 43: 3941-8 (2000)
University Of Maryland
trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: mixed dopamine D(2)/D(4) receptor antagonists as potential antipsychotic agents.
J Med Chem 43: 3923-32 (2000)
Neurogen
Radioiodinated N-(2-diethylaminoethyl)benzamide derivatives with high melanoma uptake: structure-affinity relationships, metabolic fate, and intracellular localization.
J Med Chem 43: 3913-22 (2000)
University Of Heidelberg
N,N-Diethyl-4-(phenylpiperidin-4-ylidenemethyl)benzamide: a novel, exceptionally selective, potent delta opioid receptor agonist with oral bioavailability and its analogues.
J Med Chem 43: 3895-905 (2000)
Astrazeneca R&D Montreal
New diarylmethylpiperazines as potent and selective nonpeptidic delta opioid receptor agonists with increased In vitro metabolic stability.
J Med Chem 43: 3878-94 (2000)
Astrazeneca R&D Montreal
Identification of novel inhibitors of urokinase via NMR-based screening.
J Med Chem 43: 3862-6 (2000)
Abbott Laboratories
Computational predictions of binding affinities to dihydrofolate reductase: synthesis and biological evaluation of methotrexate analogues.
J Med Chem 43: 3852-61 (2000)
Uppsala University
Design, synthesis, and X-ray crystal structure of a potent dual inhibitor of thymidylate synthase and dihydrofolate reductase as an antitumor agent.
J Med Chem 43: 3837-51 (2000)
Duquesne University
Discovery of a potent, orally bioavailable beta(3) adrenergic receptor agonist, (R)-N-[4-[2-[[2-hydroxy-2-(3-pyridinyl)ethyl]amino]ethyl]phenyl]-4-[4 -[4-(trifluoromethyl)phenyl]thiazol-2-yl]benzenesulfonamide.
J Med Chem 43: 3832-6 (2000)
Merck Research Laboratories
Synthesis of a substance P antagonist with a somatostatin scaffold: factors affecting agonism/antagonism at GPCRs and the role of pseudosymmetry.
J Med Chem 43: 3827-31 (2000)
University Of Pennsylvania
Hunting the emesis and efficacy targets of PDE4 inhibitors: identification of the photoaffinity probe 8-(3-azidophenyl)-6- [(4-iodo-1H-1-imidazolyl)methyl]quinoline (APIIMQ).
J Med Chem 43: 3820-3 (2000)
Merck Frosst Centre For Therapeutic Research
Structure-based design of novel bicyclic nonpeptide inhibitors for the src SH2 domain.
J Med Chem 43: 3815-9 (2000)
Ariad Pharmaceuticals
Characterization of (125)I-IABN, a novel azabicyclononane benzamide selective for D2-like dopamine receptors.
Synapse 38: 438-49 (2000)
University Of North Texas
Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription.
Chem Biol 7: 793-803 (2000)
Smithkline Beecham Pharmaceuticals
Cholesterol interaction with the daunorubicin binding site of P-glycoprotein.
Biochem Biophys Res Commun 276: 909-16 (2000)
Schering-Plough Research Institute
Preparation, characterization, and the crystal structure of the inhibitor ZK-807834 (CI-1031) complexed with factor Xa.
Biochemistry 39: 12534-42 (2000)
Berlex
Novel cannabinol probes for CB1 and CB2 cannabinoid receptors.
J Med Chem 43: 3778-85 (2000)
Organix
beta-Turned dipeptoids as potent and selective CCK(1) receptor antagonists.
J Med Chem 43: 3770-7 (2000)
Instituto De Qu£Mica M£Dica (Csic)
New arylpiperazine derivatives as antagonists of the human cloned 5-HT(4) receptor isoforms.
J Med Chem 43: 3761-9 (2000)
Paris-Sud University
Synthesis and opioid receptor affinity of a series of 2, 4-diaryl-substituted 3,7-diazabicylononanones.
J Med Chem 43: 3746-51 (2000)
University Of WüRzburg
Nonpeptide alpha(v)beta(3) antagonists. 1. Transformation of a potent, integrin-selective alpha(IIb)beta(3) antagonist into a potent alpha(v)beta(3) antagonist.
J Med Chem 43: 3736-45 (2000)
Merck Research Laboratories
Benzo[c]quinolizin-3-ones: a novel class of potent and selective nonsteroidal inhibitors of human steroid 5alpha-reductase 1.
J Med Chem 43: 3718-35 (2000)
Universit£
Carbonic anhydrase and matrix metalloproteinase inhibitors: sulfonylated amino acid hydroxamates with MMP inhibitory properties act as efficient inhibitors of CA isozymes I, II, and IV, and N-hydroxysulfonamides inhibit both these zinc enzymes.
J Med Chem 43: 3677-87 (2000)
Universita Degli Studi
New substituted 1-(2,3-dihydrobenzo[1, 4]dioxin-2-ylmethyl)piperidin-4-yl derivatives with alpha(2)-adrenoceptor antagonist activity.
J Med Chem 43: 3653-64 (2000)
Centre De Recherche Pierre Fabre
Replacement of glycine with dicarbonyl and related moieties in analogues of the C-terminal pentapeptide of cholecystokinin: CCK(2) agonists displaying a novel binding mode.
J Med Chem 43: 3614-23 (2000)
University Of Paris
Synthesis and SAR of new 5-phenyl-3-ureido-1,5-benzodiazepines as cholecystokinin-B receptor antagonists.
J Med Chem 43: 3596-613 (2000)
Glaxo Wellcome Medicines Research Centre
Discovery of (R)-7-cyano-2,3,4, 5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3- (phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine (BMS-214662), a farnesyltransferase inhibitor with potent preclinical antitumor activity.
J Med Chem 43: 3587-95 (2000)
Bristol-Myers Squibb Pharmaceutical Research Institute
The synthesis and biological evaluation of a novel series of phthalazine PDE4 inhibitors I.
Bioorg Med Chem Lett 10: 2235-8 (2000)
Zambon Group
Development of plasmin and plasma kallikrein selective inhibitors and their effect on M1 (melanoma) and HT29 cell lines.
Bioorg Med Chem Lett 10: 2217-21 (2001)
Kobe Gakuin University
Diphenylsulfone muscarinic antagonists: piperidine derivatives with high M2 selectivity and improved potency.
Bioorg Med Chem Lett 10: 2209-12 (2001)
Schering-Plough Research Institute
Synthesis and biological evaluation of novel piperidine carboxamide derived calpain inhibitors.
Bioorg Med Chem Lett 10: 2187-91 (2001)
Knoll
The synthesis and SAR of rhodanines as novel class C beta-lactamase inhibitors.
Bioorg Med Chem Lett 10: 2179-82 (2001)
The R. W. Johnson Pharmaceutical Research Institute
Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck II.
Bioorg Med Chem Lett 10: 2171-4 (2001)
Basf Bioresearch
Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I.
Bioorg Med Chem Lett 10: 2167-70 (2001)
Basf Bioresearch
Thermodynamic basis of resistance to HIV-1 protease inhibition: calorimetric analysis of the V82F/I84V active site resistant mutant.
Biochemistry 39: 11876-83 (2000)
The Johns Hopkins University
Structural requirements for determining the substrate affinity of peptide transporters PEPT1 and PEPT2.
Pflugers Arch 440: 679-84 (2000)
Kyoto University Hospital
A novel hepatointestinal leukotriene B4 receptor. Cloning and functional characterization.
J Biol Chem 275: 40686-94 (2000)
Schering-Plough Research Institute
8-O-Methylsclerotiorinamine, antagonist of the Grb2-SH2 domain, isolated from Penicillium multicolor.
J Nat Prod 63: 1303-5 (2000)
Korea Research Institute Of Bioscience & Biotechnology
New anabaenopeptins, potent carboxypeptidase-A inhibitors from the cyanobacterium Aphanizomenon flos-aquae.
J Nat Prod 63: 1280-2 (2000)
The University Of Tokyo
bis(2-(Acylamino)phenyl) disulfides, 2-(acylamino)benzenethiols, and S-(2-(acylamino)phenyl) alkanethioates as novel inhibitors of cholesteryl ester transfer protein.
J Med Chem 43: 3566-72 (2000)
Research Triangle Institute
Selective protection and functionalization of morphine: synthesis and opioid receptor binding properties of 3-amino-3-desoxymorphine derivatives.
J Med Chem 43: 3558-65 (2000)
Rensselaer Polytechnic Institute
Thiazoloindans and thiazolobenzopyrans: a novel class of orally active central dopamine (partial) agonists.
J Med Chem 43: 3549-57 (2000)
University Of Maastricht
2,7-Dioxo-2,3,4,5,6,7-hexahydro-1H-benzo[h][1,4]diazonine as a new template for the design of CCK(2) receptor antagonists.
J Med Chem 43: 3518-29 (2000)
James Black Foundation
Development of peptide 3D structure mimetics: rational design of novel peptoid cholecystokinin receptor antagonists.
J Med Chem 43: 3505-17 (2000)
James Black Foundation
Synthesis, stability, antiviral activity, and protease-bound structures of substrate-mimicking constrained macrocyclic inhibitors of HIV-1 protease.
J Med Chem 43: 3495-504 (2000)
The University Of Queensland
Discovery of a potent, highly selective, and orally efficacious small-molecule activator of the insulin receptor.
J Med Chem 43: 3487-94 (2000)
Merck Research Laboratories
BCX-1812 (RWJ-270201): discovery of a novel, highly potent, orally active, and selective influenza neuraminidase inhibitor through structure-based drug design.
J Med Chem 43: 3482-6 (2000)
Biocryst Pharmaceuticals
Curated by BindingDB
Curated by ChEMBL